Posaconazole 泊沙康唑 بوساكونازول Позаконазол

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Posaconazole  泊沙康唑 ,  بوساكونازول , Позаконазол
Sch-56592
4-[4-[4-[4-[[(5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one

1. Noxafil
2. SCH 56592

U.S. Patents 5,661,151; 5,703,079; and 6,958,337.

Therap-Cat: Antifungal.

CAS 171228-49-2

Molecular Formula: C37H42F2N8O4

Molecular Weight: 700.78

CAS Name: 2,5-Anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[1-[(1S,2S)-1-ethyl-2-hydroxypropyl]-1,5-dihydro-5-oxo-4H-1,2,4-triazol-4-yl]phenyl]-1-piperazinyl]phenoxy]methyl]-1-(1H-1,2,4-triazol-1-yl)-D-threo-pentitol

Additional Names: (3R-cis)-4-[4-[4-[4-[5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)tetrahydrofuran-3-ylmethoxy]phenyl]piperazin-1-yl]phenyl]-2-[1(S)-ethyl-2(S)-hydroxypropyl]-3,4-dihydro-2H-1,2,4-triazol-3-one

Syn..........Dominic De Souza, "PREPARATION OF POSACONAZOLE INTERMEDIATES." U.S. Patent US20130203994, issued August 08, 2013.

Percent Composition: C 63.41%, H 6.04%, F 5.42%, N 15.99%, O 9.13%

US5661151   EXP Jul 19, 2019  PRODUCT PATENT

US 5703079  EXP Aug 26, 2014

US8410077 EXPMar 13, 2029

US9023790 EXPJul 4, 2031

US 6958337 EXP Oct 5, 2018

US 8263600 EXPApr 1, 2022

nmr...........http://file.selleckchem.com/downloads/nmr/s125705-posaconazole-cdcl3-hnmr-selleck.pdf

1H NMR PREDICT

13C NMR PREDICT

COSY PREDICT

............................

 tetrahydroimidazole,

4

 












............

CN101824009A *

May 27, 2010

Sep 8, 2010

北京德众万全药物技术开发有限公司

Simple preparation method for posaconazole and piperazine intermediate thereof

Citing Patent	Filing date	Publication date	Applicant	Title
WO2015011224A1 *	Jul 24, 2014	Jan 29, 2015	Sandoz Ag	Improved process for the preparation of crystalline form iv of posaconazole

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सुकून उतना ही देना प्रभू, जितने से
जिंदगी चल जाये।
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1,2-Bis(2-aminophenoxy)ethyl-N,N,N',N'-acetic acid methyl ester

http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532014000100014&lng=en&nrm=iso&tlng=en

1,2-Bis(2-aminophenoxy)ethyl-N,N,N',N'-acetic acid methyl ester 4

Compound 3 (2.44 g, 0.01 mol) was dissolved in MeCN (10 mL), then (i-Pr)₂NEt (6 mL) and methyl bromoacetate (3 mL) were added to the mixture with stirring. The reaction mixture was refluxed for 24 h. After the reaction, the mixture was cooled down, poured into EtOAc (20 mL), and filtered to remove the generated white solid. The combined EtOAc filtrates were concentrated in vacuo to give an oily solid, then adding a little methanol, white solid was generated, filtered, air dried and recrystallized in MeOH to give white solid 4. Yield 87%; 

m.p. 94-95 ºC;  

¹H NMR (CDCl₃, 400 MHz) δ 6.85 (m, 8H), 4.27 (s, 4H), 4.15 (s, 8H), 3.56 (s, 12H); 

IRν/cm^-1 3067, 2993, 2951, 2921, 2888, 1748, 1596, 1509, 1173, 742, 706.

Journal of the Brazilian Chemical Society

Print version ISSN 0103-5053

J. Braz. Chem. Soc. vol.25 no.1 São Paulo Jan. 2014

http://dx.doi.org/10.5935/0103-5053.20130276 

ARTICLE

Structural study and fluorescent property of a novel organic microporous crystalline material

Zhao Cheng; Bingqin Yang^*; Meipan Yang; Binglin Zhang

Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, College of Chemistry and Materials Science, Northwest University, 710069 Xi'an, China

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सुकून उतना ही देना प्रभू, जितने से जिंदगी चल जाये। औकात बस इतनी देना, कि औरों का भला हो जाये।

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO …..FOR BLOG HOME CLICK HERE

Join me on Linkedin

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 amcrasto@gmail.com

LIONEL MY SON

He was only in first standard in school when I was hit by a deadly one in a million spine stroke called acute transverse mylitis, it made me 90% paralysed and bound to a wheel chair, Now I keep him as my source of inspiration and helping millions, thanks to millions of my readers who keep me going and help me to keep my son happy

सुकून उतना ही देना प्रभू, जितने से
जिंदगी चल जाये।
औकात बस इतनी देना,
कि औरों का भला हो जाये।

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