……
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
- Noxafil
- 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%
-
Melting Point
-
170-172 deg CO’Neil, M.J. (ed.). The Merck Index – An Encyclopedia of Chemicals, Drugs, and Biologicals. 13th Edition, Whitehouse Station, NJ: Merck and Co., Inc., 2001., p. 1365
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Solubility
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In water, 0.027 mg/L at 25 deg C (est)US EPA; Estimation Program Interface (EPI) Suite. Ver.3.12. Nov 30, 2004. Available from, as of Dec 19, 2005:http://www.epa.gov/oppt/exposure/pubs/episuitedl.htm
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
1H NMR PREDICT
13C NMR PREDICT
COSY PREDICT
| 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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