WO2008065490A3 - Process for the preparation of atazanavir - Google Patents
Process for the preparation of atazanavir Download PDFInfo
- Publication number
- WO2008065490A3 WO2008065490A3 PCT/IB2007/003470 IB2007003470W WO2008065490A3 WO 2008065490 A3 WO2008065490 A3 WO 2008065490A3 IB 2007003470 W IB2007003470 W IB 2007003470W WO 2008065490 A3 WO2008065490 A3 WO 2008065490A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- methoxycarbonyl
- atazanavir
- preparation
- leucine
- tert
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to a process for the preparation of Atazanavir, which comprises reacting the hydrochloride salt of compound (6) with N-methoxycarbonyl-L-tert-leucine, the removal of the benzyloxycarbonyl group and the reaction with methoxycarbonyl chloride. The process is particularly advantageous in that it allows to use reduced amounts of N-methoxycarbonyl-L-tert-leucine and avoids the use of unstable intermediates.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP07848883A EP2094661A2 (en) | 2006-11-28 | 2007-11-13 | Process for the preparation of atazanavir |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06024597A EP1930324A1 (en) | 2006-11-28 | 2006-11-28 | Process for the preparation of atazanavir |
EP06024597.4 | 2006-11-28 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2008065490A2 WO2008065490A2 (en) | 2008-06-05 |
WO2008065490A3 true WO2008065490A3 (en) | 2008-08-14 |
Family
ID=37906960
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IB2007/003470 WO2008065490A2 (en) | 2006-11-28 | 2007-11-13 | Process for the preparation of atazanavir |
Country Status (2)
Country | Link |
---|---|
EP (2) | EP1930324A1 (en) |
WO (1) | WO2008065490A2 (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2272830A1 (en) | 2009-06-18 | 2011-01-12 | Esteve Química, S.A. | Preparation process of an antivirally heterocyclic azahexane derivative |
EP2542527A2 (en) | 2010-03-01 | 2013-01-09 | Lupin Limited | Process for the preparation of atazanavir sulfate substantially free of diastereomers |
US20140343290A1 (en) | 2011-07-27 | 2014-11-20 | Rakesh Kumar Singh | Process for the preparation of atazanavir or its bisulfate salt |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5849911A (en) * | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
-
2006
- 2006-11-28 EP EP06024597A patent/EP1930324A1/en not_active Withdrawn
-
2007
- 2007-11-13 EP EP07848883A patent/EP2094661A2/en not_active Withdrawn
- 2007-11-13 WO PCT/IB2007/003470 patent/WO2008065490A2/en active Application Filing
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5849911A (en) * | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
Non-Patent Citations (3)
Title |
---|
BOLD, GUIDO ET AL: "New Aza-Dipeptide Analogs as Potent and Orally Absorbed HIV-1 Protease Inhibitors: Candidates for Clinical Development", JOURNAL OF MEDICINAL CHEMISTRY , 41(18), 3387-3401 CODEN: JMCMAR; ISSN: 0022-2623, vol. 41, 1998, pages 3387 - 3401, XP002338294 * |
XU, ZHONGMIN ET AL: "Process Research and Development for an Efficient Synthesis of the HIV Protease Inhibitor BMS-232632", ORGANIC PROCESS RESEARCH & DEVELOPMENT , 6(3), 323-328 CODEN: OPRDFK; ISSN: 1083-6160, vol. 6, 2002, pages 323 - 328, XP002429422 * |
ZHANG, HUIPING ET AL: "A facile and efficient synthesis of d3-labelled Reyataz", JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS , 48(14), 1041-1047 CODEN: JLCRD4; ISSN: 0362-4803, vol. 48, 2005, pages 1041 - 1047, XP002429423 * |
Also Published As
Publication number | Publication date |
---|---|
WO2008065490A2 (en) | 2008-06-05 |
EP1930324A1 (en) | 2008-06-11 |
EP2094661A2 (en) | 2009-09-02 |
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