4 - methoxy benzoin

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DESLORATIDINE

[0052] Table 1, desloratadine sample IH-NMR data of the DMS0_d6

[0055] The desloratadine 1H spectra of the samples were assigned:
[0056] (I) 1H spectra show that there are 10 groups of hydrogen from low field to high field integral hydrogen ratio was 1: 1: 1: 1: 1: 1: 2: 4:
2: 4, and desloratadine structure match.
[0057] (2) δ 8.334 处 hydrogen as a set of double doublet, number of protons is I, attributed to two hydrogen;
[0058] (3) δ 7.560 处 hydrogen as a set of double doublet, number of protons is I, attributed to four hydrogen;
[0059] (4) δ 7.282 处 doublet hydrogen as a group, the number of protons is I, 12 attributed to hydrogen.
[0060] (5) δ 7.198 处 hydrogen as a set of double doublet, number of protons is I, 14 attributed to hydrogen;
[0061] (6) δ 7.174 处 hydrogen as a set of double doublet, number of protons is I, attributed to three hydrogen;
[0062] (7) δ 7.064 处 doublet hydrogen as a group, the number of protons is I, 15 attributed to hydrogen;
[0063] (8) δ 3.314 处 hydrogen as a group multiplet, 2 protons attributable to 10 hydrogen;
[0064] (9) δ 2.831,2.554 hydrogen groups at multiplet, protons of 4, 18, 20, the home position is hydrogen;
[0065] (10) δ 2.819 处 hydrogen as a group multiplet, 2 protons attributable to 11 hydrogen;
[0066] (11) δ 2.108 处 hydrogen as a single peak, the number of protons is I, home to 19 active hydrogen;
[0067] (12) δ 2.205, 2.002 处 two hydrogen multiplet, protons of 4, 17, 21 bits attributed to hydrogen; [0068] From the foregoing, 1H-NMR spectrum data and the resulting product in this embodiment is of he will be loratadine same structure as the target product.

 http://www.google.com/patents/CN103755682A?cl=en





 
The value of substituted 3-picoline precursors is illustrated in the synthesis of clarinex (1.22, Desloratadine, Scheme 5), a dual antagonist of platelet activating factor (PAF) and of histamine used in the treatment of allergies. This compound consists of a highly functional tricyclic core with an unsaturated linkage to a pendant piperidine ring. The picoline derivative 1.23 is first treated with two equivalents of n-butyllithium (n-BuLi) followed by alkylation with benzyl chloride to give the chain elongated adduct [27]. The tert-butylamide 1.24 is then dehydrated with phosphorous oxychloride at elevated temperatures to yield the nitrile derivative 1.25. Introduction of the piperidine ring is achieved by utilisation of the appropriately substituted Grignard reagent 1.26. A Friedel–Crafts type acylation promoted by either triflic acid or polyphosphoric acid (PPA) furnishes the tricyclic structure 1.28 which upon N-demethylation affords clarinex (1.22).

 http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-9-265
 
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Lipiar 120493 from Lipiar Khan Mohammad Osman Goni


Desloratadine

CAS Registry Number: 100643-71-8

CAS Name: 8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine

Additional Names: descarboethoxyloratadine

Manufacturers' Codes: Sch-34117

Trademarks: Clarinex (Schering-Plough)

Molecular Formula: C19H19ClN2

Molecular Weight: 310.82

Percent Composition: C 73.42%, H 6.16%, Cl 11.41%, N 9.01%

Literature References: Nonsedating-type histamine H1-receptor antagonist; active metabolite of loratadine, q.v. Also inhibits generation and release of inflammatory mediators from basophils and mast cells. Prepn: D. P. Schumacher et al., EP 208855; F. J. Villani, J. K. Wong, US 4659716 (both 1987 to Schering). GLC determn in plasma: R. Johnson et al., J. Chromatogr. B 657, 125 (1994). Pharmacology: W. Kreutner et al., Arzneim.-Forsch. 50, 345 (2000). Series of articles on clinical efficacy in rhinitis, asthma and urticaria: Allergy 56, Suppl. 65, 1-32 (2001). Review of pharmacology, pharmacokinetics and clinical efficacy: R. S. Geha, E. O. Meltzer, J. Allergy Clin. Immunol. 107, 751-762 (2001); D. K. Agrawal, Expert Opin. Invest. Drugs 10, 547-560 (2001).

Properties: Crystals from hexane, mp 150-151°. Slightly sol in water; very sol in ethanol, propylene glycol.

Melting point: mp 150-151°

Therap-Cat: Antihistaminic.

Keywords: Antihistaminic; Tricyclics; Other Tricyclics.

 

CETIRIZINE DIHYDROCHLORIDE

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MIDAZOLAM HYDROCHLORIDE

Title: Midazolam CAS Registry Number: 59467-70-8 CAS Name: 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine Molecular Formula: C18H13ClFN3 Molecular Weight: 325.77 Percent Composition: C 66.36%, H 4.02%, Cl 10.88%, F 5.83%, N 12.90% Literature References: Short-acting deriv of diazepam, q.v. Prepn: R. I. Fryer, A. Walser, DE 2540522; eidem, US 4280957 (1976, 1981 both to Hoffmann-La Roche); A. Walser et al., J. Org. Chem. 43, 936 (1978). HPLC determn in plasma: S. L. Eeckhoudt et al., J. Chromatogr. B 710, 165 (1998). Toxicity data: L. Pieri et al., Arzneim.-Forsch. 31, 2180 (1981). Series of articles on pharmacology, metabolism, pharmacokinetics, clinical experience: ibid. 2177-2288; Br. J. Clin. Pharmacol. 16, Suppl. 1, 1S-199S (1983). Review of pharmacology and therapeutic use: J. W. Dundee et al., Drugs 28, 519-543 (1984); in treatment of status epilepticus: D. F. Hanley, J. F. Kross, Clin. Ther. 20, 1093-1105 (1998). Clinical evaluation for intranasal treatment of febrile seizures in children: E. Lahat et al., Br. Med. J. 321, 83 (2000). Properties: Colorless crystals from ether/methylene chloride/hexane, mp 158-160°. uv max (2-propanol): 220 nm (e 30000). Melting point: mp 158-160° Absorption maximum: uv max (2-propanol): 220 nm (e 30000)   Derivative Type: Maleate CAS Registry Number: 59467-94-6 Manufacturers' Codes: Ro-21-3981/001 Trademarks: Dormicum (Roche) Molecular Formula: C18H13ClFN3.C4H4O4 Molecular Weight: 441.84 Percent Composition: C 59.80%, H 3.88%, Cl 8.02%, F 4.30%, N 9.51%, O 14.48% Properties: Crystals from ethanol/ether, mp 114-117° (solvated). LD50 in male mice (mg/kg): 760 orally; 86 i.v. (Pieri). Melting point: mp 114-117° (solvated) Toxicity data: LD50 in male mice (mg/kg): 760 orally; 86 i.v. (Pieri)   Derivative Type: Hydrochloride CAS Registry Number: 59467-96-8 Manufacturers' Codes: Ro-21-3981/003 Trademarks: Hypnovel (Roche); Versed (Roche) Molecular Formula: C18H13ClFN3.HCl Molecular Weight: 362.23 Percent Composition: C 59.68%, H 3.90%, Cl 19.57%, F 5.24%, N 11.60% Properties: Sol in aqueous solns.   NOTE: This is a controlled substance (depressant): 21 CFR, 1308.14. Therap-Cat: Anesthetic (intravenous); anticonvulsant; sedative, hypnotic. Keywords: Anesthetic (Intravenous); Anticonvulsant; Sedative/Hypnotic; Benzodiazepine Derivatives.

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10-benzoiloxy-6,8,9-trihydroxy-thymol isobutyrate

The dichloromethane extract of A. glabrata leaves was fractionated by column chromatography affording a pure compound 10-benzoiloxy-6,8,9-trihydroxy-thymol isobutyrate (1). The mass spectrum indicated a molecular ion at m/z 388 in agreement with the molecular formula C₂₁H₂₄O₇, m/z 370 (12%) [M-H₂O]⁺, 178 (46%), 165 (43%), 150 (15%), 137 (5 %), 122 (23%), 105 (100%), 91 (5%), 71 (40%). The ¹H NMR spectrum (Figure 2) indicates the presence of a benzoate group at 7.98, 7.55 and 7.40 ppm; singlets at 6.65 and 6.58 ppm for 2 and 5 aromatic hydrogens, respectively. The signals for the isopropyl group at 2.52 and 1.09 ppm. A singlet at 4.64 ppm for two hydrogens of methylene group in the 10-position of the molecule and the hydrogens of methylene group in C-9 were observed as a doublet each at 4.56 and 4.49 ppm. The ¹³C NMR spectrum (Table 1) was in agreement with the proposed structure. Eleven thymol derivatives have been obtained by Bohlmann et al 1977 from A. glabrata, but all of them differ from the new thymol derivative 1.

General

NMR measurements, including DEPT experiments, were performed at 400 MHz for ¹H and 100 MHz for ¹³C on a Varian Mercury Plus 400 spectrometer, using CDCl₃ as the solvent and TMS as internal reference. Mass spectra were recorded at 20 eV on a Hewlett-Packard 5989B Series II Plus spectrometer adapted to a HP 5890 gas chromatography. Column chromatography was carried out on Merck silica gel grade 60 (70-230 mesh).

Plant material

Specimens of Ageratina glabrata (Kunth) R.M. King & H. Rob., Asteraceae, were collected on January 4, 2006 near km 191 of México-Morelia state road No.15, in the municipality of San José de la Cumbre, State of Michoacán, México (N 19º40'859'', W 100º50'423'' and 2,234 meters above sea level). A voucher specimen (No. 188319) is deposited at the Herbarium of the Instituto de Ecología, A.C., Centro Regional del Bajío, Pátzcuaro, Michoacán, Mexico, where Prof. Jerzy Rzedowski kindly identified the plant material (Figure 1).

Preparation of plant extract

Air-dried leaves of A. glabrata (200 g) were extracted with CH₂Cl₂ (1.5 L) at room temperature for three days, three consecutive times. Filtration and evaporation of the extract afforded green viscous oil (19 g).

Isolation of the thymol derivative (1) from dichloromethane extract

The dichloromethane extract (0.5 g) was chromatographed on silica gel column using n-hexane and ethyl acetate mixture of increasing polarity, and finally pure ethyl acetate. Elution with hexane:EtOAc (9:1) afforded a mixture of thymol derivatives. The sub-fraction 30-32 (100 mg) was subjected to rechromatography on silica gel (5 g). Elution with n-hexane-AcOEt (8:2) afforded pure 10-benzoiloxy-6,8,9-trihydroxy-thymol isobutyrate (1) (20 mg). Identification was supported by spectroscopic analyses.

Revista Brasileira de Farmacognosia

Print version ISSN 0102-695X

Rev. bras. farmacogn. vol.21 no.5 Curitiba Sept./Oct. 2011  Epub Sep 02, 2011

http://dx.doi.org/10.1590/S0102-695X2011005000158 

Analgesic effect of leaf extract from Ageratina glabrata in the hot plate test

Guadalupe García P^I; Edgar García S^III; Isabel Martínez G^I; Thomas R. F. Scior^II; José L Salvador ^III; Mauro M Martínez P^III; Rosa E. del Río^*,III

^ILaboratorio de Neuroquímica, Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, Mexico
^IILaboratorio de Farmacomodelaje, Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Puebla, Mexico
^IIIInstituto de Investigaciones Químico-Biológicas, Universidad Michoacana de San Nicolás de Hidalgo, Morelia, Mexico

*Correspondence 
Rosa E. del Río 
Instituto de Investigaciones Químico-Biológicas, Universidad Michoacana de San Nicolás de Hidalgo. 
Ed. B-1, C.U. Morelia, Mich. ,58030, Mexico. 
ndelrio@umich.mx 
Tel. +52 443 3265790 ext. 102; 3265790 ext. 103.

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