DR ANTHONY MELVIN CRASTO,WorldDrugTracker, helping millions, A 90 % paralysed man in action for you, I am suffering from transverse mylitis and bound to a wheel chair, With death on the horizon, nothing will not stop me except God................DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 25Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK GENERICS at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution

Wednesday, 1 June 2016

Intensified biocatalytic production of enantiomerically pure halophenylalanines from acrylic acids using ammonium carbamate as the ammonia source

Catal. Sci. Technol., 2016, Advance Article DOI: 10.1039/C6CY00855K, Communication
Nicholas J. Weise, Syed T. Ahmed, Fabio Parmeggiani, Elina Siirola, Ahir Pushpanath, Ursula Schell, Nicholas J. Turner An industrial-scale method employing a phenylalanine ammonia lyase enzyme

Intensified biocatalytic production of enantiomerically pure halophenylalanines from acrylic acids using ammonium carbamate as the ammonia source

*Corresponding authors
aManchester Institute of Biotechnology & School of Chemistry, University of Manchester, 131 Princess Street, Manchester, UK E-mail: nicholas.turner@manchester.ac.uk
bJohnson Matthey Catalysts and Chiral Technologies, 28 Cambridge Science Park, Milton Road, Cambridge, UK
Catal. Sci. Technol., 2016, Advance Article
DOI: 10.1039/C6CY00855K
SEE
An intensified, industrially-relevant strategy for the production of enantiopure halophenylalanines has been developed using the novel combination of a cyanobacterial phenylalanine ammonia lyase (PAL) and ammonium carbamate reaction buffer. The process boasts STYs up to >200 g L−1 d−1, ees ≥ 98% and simplified catalyst/reaction buffer preparation and work up. STR1 STR1 STR1 STR1 ///////Intensified, biocatalytic production, enantiomerically pure, halophenylalanines, acrylic acids, ammonium carbamate, ammonia source





Mnemba,  Indian Ocean,  Zanzibar,
Tanzania

.


Image result for Mnemba,
Map of Mnemba Island
Mnemba Island
Island in Tanzania
Mnemba Island is a single small island located about 3 km off the northeast coast of Unguja, the largest island of the Zanzibar Archipelago, Tanzania, opposite Muyuni Beach. Wikipedia
Max length: 6.6 km
 
 
 
 
 

 

 

 

 
 


fisherman
fishing boats
mnemba in the distance
Within minutes, we were whisked away to Zanibar’s private gem and warmly welcomed by the GM, our butler, and a few other members of their team with cool towels and cocktails. I was hesitant to let my shoes go, but it was the best thing ever! This is truly a barefoot paradise. Mike, the GM showed us around & finally to our banda. (the individual rooms are called bandas) On our first trip during August we stayed in banda 11 on the furthest point of the island with the most magnificent sunrise view. This time, during January we stayed in banda 4 which was wonderful for that time of year as it is quite windy.
arrival
sunrise from banda
The banda takes some getting used to as it has a indoor-outdoor feel, but is private. Each banda is very secluded and don’t worry, you won’t be caught walking around naked, if you choose to. The only time our butler would visit (without us asking for his assistance) is to bring us coffee in the morning at a desired time, which we would give him the night before. We had Rajab and Christopher as our butlers, both made us feel at home.
banda relaxing area
banda bathroom
banda closet
Almost everything in the room is natural and blends in perfectly with the surroundings. There is no television or telephone available – but there is Wi-Fi. I don’t need to say much about the bandas, its perfect and the pictures speak for themselves.
the banda
view from banda
to the bathroom from the banda  bedroom
The resort doesn’t have a gym, but you are provided with a gym in a bag. Honestly speaking, who needs that when you’re on a private island? A therapist who is also a yoga master is on hand to offer you treatments in the comfort of your banda. Breakfast and Lunch is served at the dining area – whenever you wish to eat, with a different menu each day. The chef is very flexible, if there is something you would like to eat or change on their menu, they are ready to oblige.
menu board
breakfast and lunch area
breakfast view
Let’s talk food – absolutely DELICIOUS to say the least. Chefs Ishan and Jaco come out each morning to give you the run down of the menu for the day and that’s when you have an opportunity to alter anything you wish to. The menu is predominantly seafood, and you cannot get anything fresher! The best fish I’ve eaten, was at Mnemba.
lunch
coconut sorbet
Each evening at sunset, sun chairs are set outside the Banda facing the sunset and your butler brings you a cocktail or drink of your choice. Absolute bliss!
sunset cocktails
sunset1
sunset2
Dinner is usually on the beach – but if the timing of your stay is good, you will get to experience a beach barbeque (Braai). The pre dinner drinks on the beach, lit up by candles and lamps is so inviting! You will also get to experience the Calamari Brothers, a singing duo – Mike the GM and Jaco, the head chef. The two came together by chance and ended up getting a name!
barbeque dinner setup
Sitting by the beach, listening to music with drink in hand under moonlight in good company is just perfect. Drinks usually start in the bar from about 7pm and dinner is served at 8. This is when you get to meet other guests and the hosts (Members of their team), are always there to engage you. There are only 12 bandas, so there will be a maximum of 24 guests – most of the time we felt like we were on our very own island.
the bar
It is by far one of the most romantic places I have ever visited. There aren’t too many activities on offer – but you can snorkel, dive and swim with the dolphins and it’s all included in the rate. I went on some amazing snorkeling expeditions with Matt. We would go out on our own and explore. Mnemba has some of the most beautiful, untouched reefs I have ever seen. My husband completed his open water dive course with Marie and he could not have had a better teacher. The island also has its own house reef, so you can swim out and snorkel on your own.
Back from diving
Snorkeling with Matt
The Dive centre
Mnemba is small – you can walk around it in about 25min and I loved taking daily walks exploring on my own. On one side of the island, during low tide, the sea would recede up to 200m! The natural beauty of this island is unmatched.
low tide2
beauty
around the island
As you walk around you may notice signboards in the sand with dates on it. One of And Beyond Safari’s priorities is conservation and Mnemba is one of only two protected nesting sites in Zanzibar for the endangered green turtle. If you are lucky enough, you will witness the hatching process and their mini voyage to the ocean. It was such a beautiful experience, the turtles can barely see, but can sense the sea. It’s incredible how they gravitate toward the ocean! It’s best not touch them if you are not wearing gloves as our bacteria can cause them illnesses. We did meet a little guy with a leg that wasn’t fully formed, but that didn’t stop him, he took longer than everyone else, but he made it!
baby turtle
turtles making their way to the beach
turtle nest
 baby turtles
As you explore the island you will also meet little deer-like animals, the suni and ader dyker, both species of antelope. Being some of the rarest in Africa, they are protected on the island and allowed to breed. I was hoping to catch sight of the coconut crab but I don’t think he wanted to see me.
in the forest
suni
The island seemed to have a micro climate. Mnemba had clear skies everyday, while the main island of Zanzibar, just across from us, would be cloudy and rainy, it was very strange but very special! I can say so much more, but it would never do justice. Hopefully my pictures show you the true magic of this island. I can’t wait to return! So long Mnemba, till we meet again.
Mnemba from Mtoni shore




  ///////////////

Дапипразол Dapiprazole

Dapiprazole.svg


Dapiprazole
CAS 72822-12-9
HCL SALT 72822-13-0
5,6,7,8-Tetrahydro-3-(2-(4-(O-tolyl)-1-piperazinyl)ethyl)-S-triazolo(4,3-a)pyridine


Dapiprazole (Rev-Eyes) is an alpha blocker. It is used to reverse mydriasis after eye examination.[1]
Used in the treatment of iatrogenically induced mydriasis produced by adrenergic (phenylephrine) or parasympatholytic (tropicamide) agents used in certain eye examinations.
Dapiprazole is an alpha-adrenergic blocking agent. It produces miosis by blocking the alpha-adrenergic receptors on the dilator muscle of the iris. Dapiprazole produces no significant action on ciliary muscle contraction and thus, there are no changes in the depth of the anterior chamber of the thickness of the lens. It does not alter the IOP either in normal eyes or in eyes with elevated IOP. The rate of pupillary constriction may be slightly slower in clients with brown irises than in clients with blue or green irises.
Dapiprazole acts through blocking the alpha1-adrenergic receptors in smooth muscle. It produces miosis through an effect on the dilator muscle of the iris and does not have any significant activity on ciliary muscle contraction and, therefore does not induce a significant change in the anterior chamber depth or the thickness of the lens.
Oral LD50 is 1189-2100 mg/kg in mice, rats and rabbits.

Brief background information

Salt ATC formula MM CASE
N05AX
S01EX02
C19H27N5 325.46 g / mol 72822-12-9
monogïdroxlorïd N05AX
S01EX02
C19H27N5 · HCl 361.92 g / mol 72822-13-0

Application

  • antipsihoticheskoe means
  • in the treatment of glaucoma

Classes substance

  • Piperazinы
    • 1,2,4-triazolo [4,3-a] piridinы

Synthesis

STR1


Синтез a)


Scheme illustration:By cyclization of O-methylvalerolactam (I) with 3-(4-o-tolyl-1-piperazinyl) propionic acid hydrazide (II) in refluxing xylene, followed by a treatment with ethanolic HCl.

FR 2423221; GB 2020269; JP 54157576; NL 7902489; US 4252721



Acylation of (1-methylcyclopropyl)guanidine (IV) with 3-bromo-5-chlorothiophene-2-sulfonyl chloride (III) under Schotten-Baumann conditions afforded the sulfonyl guanidine (V). This was cyclized to the desired thienothiadiazine upon treatment with Cs2CO3 and Cu2O in boiling butanol.


In a different method, (1-methylcyclopropyl)guanidine (I) is acylated by 3-bromo-5-chlorothiophene-2-sulfonyl chloride (II) to produce the sulfonyl guanidine (III). Intramolecular cyclization of (III) in the presence of Cu2O and Cs2CO3 leads to the title thienothiadiazine derivative. Similarly, acylation of guanidine (I) with 3,5-dichlorothiophene-2-sulfonyl chloride (IV) provides sulfonyl guanidine (V), which is then cyclized in the presence of Cu2O and Cs2CO3.


In an alternative method, sulfonylation of N-isopropylguanidine (V) with 2,5-dichlorothiophene-3-sulfonyl chloride (IV) produced the sulfonyl guanidine (VI). This was then cyclized to the title compound by treatment with copper bronze and potassium carbonate in boiling DMF……..WO 0102410

Trade names

country Tradename Manufacturer
Germany Remidrial winegrower
Italy Glamidolo Angelini, 1987
Ukraine no no

Formulations

  • eyedrops 50 mg / 10 ml (5%) (hydrochloride)

References

  • DE 2 915 318 (Angelini; appl. 14.4.1979; I-prior. 18.4.1978).
  • US 4 307 095 (Angelini; 22.12.1981; prior. 29.3.1979, 29.8.1980; I-prior. 18.4.1978).
  • US 4 307 096 (Angelini; 22.12.1981; prior. 29.3.1979, 29.8.1980; I-prior. 18.4.1978).
  • US 4 325 952 (Angelini; 20.4.1982; prior. 29.3.1979, 29.8.1980; I-prior. 18.4.1978).
  • BE 877 161 (Angelini; appl. 21.6.1979).

References

  1. Doughty, Michael J.; Lyle, William M. (May 1992). “A Review of the Clinical Pharmacokinetics of Pilocarpine, Moxisylyte (Thymoxamine), and Dapiprazole in the Reversal of Diagnostic Pupillary Dilation”. Optometry & Vision Science 69 (5).
  2. US 4 307 096 (Angelini; 22.12.1981; prior. 29.3.1979, 29.8.1980; I-prior. 18.4.1978).
  3.  US 4 325 952 (Angelini; 20.4.1982; prior. 29.3.1979, 29.8.1980; I-prior. 18.4.1978).
  4. BE 877 161 (Angelini; appl. 21.6.1979).
  5. DE 2 915 318 (Angelini; appl. 14.4.1979; I-prior. 18.4.1978).
  6. US 4 307 095 (Angelini; 22.12.1981; prior. 29.3.1979, 29.8.1980; I-prior. 18.4.1978).

Structural formula


UV- Spectrum

Conditions : Concentration – 1 mg / 100 ml
The solvent designation schedule methanol
water
0.1М HCl
0.1M NaOH
maximum absorption 235 nm 235 nm 234 nm There
decay
212 179 172
e 7650 6450 6200

IR – spectrum

Wavelength (μm)
Wave number (cm -1 )
 STR1
STR1

References

  • UV and IR Spectra. H.-W. Dibbern, R.M. Muller, E. Wirbitzki, 2002 ECV
  • NIST/EPA/NIH Mass Spectral Library 2008
  • Handbook of Organic Compounds. NIR, IR, Raman, and UV-Vis Spectra Featuring Polymers and Surfactants, Jr., Jerry Workman. Academic Press, 2000.
  • Handbook of ultraviolet and visible absorption spectra of organic compounds, K. Hirayama. Plenum Press Data Division, 1967.

Dapiprazole
Dapiprazole.svg
Systematic (IUPAC) name
3-{2-[4-(2-methylphenyl)piperazin-1-yl]ethyl}-5,6,7,8-
tetrahydro-[1,2,4]triazolo[4,5-a]pyridine
Clinical data
AHFS/Drugs.com Consumer Drug Information
MedlinePlus a601043
Pregnancy
category
  • B
Routes of
administration
Topical (eye drops)
Legal status
Legal status
  • ℞ (Prescription only)
Pharmacokinetic data
Bioavailability Negligible when administered topically
Identifiers
CAS Number 72822-12-9 Yes
ATC code S01EX02 (WHO)
PubChem CID 3033538
IUPHAR/BPS 7155
DrugBank DB00298 Yes
ChemSpider 2298190 Yes
UNII 5RNZ8GJO7K Yes
KEGG D07775 Yes
ChEBI CHEBI:51066 Yes
ChEMBL CHEMBL1201216 
Chemical data
Formula C19H27N5
Molar mass 325.451 g/mol
//////Дапипразол ,  Dapiprazole, AF-2139, Remydrial, Rev-Eyes, Reversil, Glamidolo
n1nc(n2c1CCCC2)CCN4CCN(c3ccccc3C)CC4




BURMA


 


HERE ARE MY 10 REASONS WHY YOU SHOULD PACK YOUR BAGS AND HEAD TO BURMA!

01: The People

For true hospitality, travel to Burma
In my travel experience, out of all the Asians I have met, the Burmese are the kindest, most friendly people who are willing to go above and beyond to make friends with you, help you out and make sure you are having a great time in their country. They always seem to be happy, smiling and keen to practice their English over a glass of tea! They can be quite a shy people as they are extremely polite, kids tend to be the exception to the rule – they will always run up to you to practice their English and unlike the rest of Asia, I was never once hassled by locals for money. The Burmese left a lasting impression on me; I felt that I could truly trust them and I made some incredible connections with locals I met whilst travelling there.
Local kids in Burma Myanmar
 

02: Insane Temple Ruins

Get lost in some of the biggest temple ruins in the world
When most people think of lost cities they immediately think of Angor Wat in Cambodia or maybe Hampi in India but the ruins of Bagan in central Burma are without a doubt the most stunning, least touristey, ruins I have ever seen. I spent an incredible few days exploring by bike, watching the sun set over Bagan’s temple studded plains and making friends with the local kids out to practice their English. For the true adventurer, you can head even deeper into the country’s largely unexplored regions and visit the stunning temple ruins at Mrauk Au, you will probably have them all to yourself.

03: Real Exploring

Discover the Asia of 100 years ago
Burma is an absolutely massive country and there are many hidden gems in this astounding country which only the locals will know about. It is extremely easy to get off the beaten track and to have temples, ruins, mountains and caves all to yourself. When backpacking in Burma, I felt like I had stepped back 100 years in to the past, I felt like a proper explorer. The people who I met in remote communities in the Shan highlands had often not seen another westerner for months or even years, this is prime exploring territory.  Whilst exploring the south of the country I came across a huge field of painted Buddha statues, some were cracked and covered by jungle, others looked freshly painted. Who built, painted and maintained them? I have no idea. This is why I love Burma. An unexpected field of Buddhas in the Jungle.

04: Trekking

Take to the hills and meet awesome people
Trekking in Burma is a relatively new activity but already tour agencies are springing up to cater for adventourous backpackers. Most backpackers opt for a two day trek around the stilt villages of Inle Lake but for a real experience; head deep into the Shan highlands or South to Hp-Pan. Here you can summit jungle clad limestone peaks, many of which are topped by small monastries, and soak in some spectacular views. Trekking in Burma is a really amazing experience; I met colourful freshwater crabs, hiked through mist draped forests and shared tea with novice monks who spoke no English but always seemed happy to see me.

05: Monks

Spiritual-esque discussions galore
Speaking of Monks, it’s pretty hard to travel in Burma without meeting a few! I had some amazing discussions with monks I met in temples, on buses, in the street or even whilst riding my bicycle. I was told by a monk that 1% of Burma’s entire population are monks and they certainly seem to be everywhere. Whilst trekking I met a shy monk working on repairing a temple wall, we chatted for a while and I spent an hour helping him, he offered me tea and allowed me to take his photograph. I came away with a much richer understanding of what Buddhism is all about. The monks are a friendly bunch and would often ask me all kinds of questions about life outside Burma, spirituality and even football!
 Aspiring Monks in Burma Myanmar The Broke Backpacker Meeting Monks in Burma


 

06: Food

 “Really? The food’s OK?” I hear you ask…
The food is better than OK, Burmese cuisine is some of the best in Asia. Sure, there may not be many Burmese restaurants outside of Burma but that’s largely because the country has been shut off from the rest of the world for so long. The food is an eclectic mix of Thai, Chinese and Indian cuisine and basically includes all the best bits from Thai, Chinese and Indian dishes. Check these tasty, one of a kind, dishes out:
– Gyin Thohk – tasty ginger salad with sesame seeds.
– Fruit Shakes – Keep an eye out for creamy avocado and banana shakes around Inle Lake
– Kat Kyi Hnyat – The Burmese answer to Pad Thai, a gorgeous coastal dish of rice noodles with seafood, meats, raw bean sprouts and fried eggs.
– Danbauk – A tasty Indian inspired curry served with mango pickle, fresh mint and green chili.
– Shan Tofu – Do not miss this awesome home-made tofu from the Shan highlands.

07: Cheap Beer!

The Broke Backpacker drinking cheap beer in Burma Myanmar Beer for 50 cents?!
I have made it a personal mission to sample as many local beers throughout the world as I possibly can… so far, Myanmar Beer is without a doubt my favourite brand. For just 50 cents, you can have a cool, refreshing, tap drawn beer in a iced glass. For five bucks, you can get well and truly merry. Mandalay Beer makes a tasty alternative if you get sick of Myanmar Beer but I can guarantee you won’t.

08: Stunning Islands & Beaches

Burma has a hidden paradise of unexplored beaches and islands
Most Backpackers are not yet aware that Burma has some of the world’s most beautiful beaches and islands. Until recently, these palm-fringed, white sand playgrounds were off limits unless you had a super-yacht handy but this is changing fast and every week more and more restrictions are being lifted. Now is the perfect time to travel to Burma and hunt for your dream island; think coral blue waters, coconut cocktails and perfect sandy beaches, the opportunities are endless. There are over 800 islands in Burma’s Mergui archipelago which are currently empty, making this the perfect opportunity to head out on a kayak or boat and discover paradise in the ocean.

Adventuring to Burma's Mergui archipelago



09: Caves

Discover cavernous underground temples filled with Buddha images
When travelling, I’m always looking for adventurous ways to keep myself busy, whether it’s living in a cave with a Bedouin or mountain biking through the jungles of Laos. In Burma, there is a ton of activities for the adventurous traveller but one of the best has got to be exploring some of the huge caves which pockmark the country. Many of these are not covered by any guidebook, it’s simply a case of asking around and seeing if there are any cool caves nearby. One of the biggest which I visited, in the South of the country, was filled with huge Buddha images and statues as well as some beautiful rock formations. I walked through it for over an hour, it must have been about three kilometres long, before I emerged on the other side to find a hidden lake framed by a backdrop of limestone mountains; to this day it is still one of the most beautiful things I have discovered whilst backpacking.


10: It’s changing fast

Now is the time to go!
Burma is well and truly back on the Backpacker map and in 2014 it has become THE place to go. I was lucky enough to first visit in 2012 and I met perhaps a dozen backpackers in my entire time there. These days, more and more backpackers are tagging Burma on to the classic Thailand – Laos – Vietnam – Cambodia route, and rightly so! However, as the country continues to open up and as investment and travelers continue to pour in it is only a matter of time before some of Burma’s most enchanting attractions become diluted. Luckily, the country is so big that there is plenty of room and plenty of wild places left for backpackers to explore. Do not hesitate; visit this incredible land now, meet the wonderful people, have a beer or three and explore till your heart’s content.
 
…AND NOW? PACK YOUR BACKPACK, BOOK YOUR FLIGHT AND GET OUT THERE!!
Need some more information? Check out this travel guide I wrote based on my travels in Burma.