Wockhardt, WO 2007023507, N-[[3-[3,5-difluoro-4-[4-(tetrazol-2-yl)piperidin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide

Cas 928156-95-0,

Acetamide, N-​[[(5S)​-​3-​[3,​5-​difluoro-​4-​[4-​(2H-​tetrazol-​2-​yl)​-​1-​piperidinyl]​phenyl]​-​2-​oxo-​5-​oxazolidinyl]​methyl]​-

N-[[3-[3,5-difluoro-4-[4-(tetrazol-2-yl)piperidin-1-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide

Example- 14 and 15

(S)-N- { 3- [4-(4-(2H-tetrazol-2-yl)-piperidin- 1 -yl)-3 , 5-difluorophenyl] -2-oxo-oxazolidin-

5-ylmethyl }-acetamide and

(S)-N- { 3- [4-(4-(l H-tetrazol- 1 -yl)-piperidin- 1 -yl)-3 , 5-difluorophenyl] -2-oxo-oxazolidin-

5-ylmethyl }-acetamide

and

A mixture of (S)-N-{3-[4-methanesulphonyloxy piperidin-l-yl)-3,5-difluorophenyl]-2- oxo-oxazolidin-5-ylmethyl}-acetamide (1.12 mM), tetrazole (1.68 mM), and K₂CO₃ (1.68 mM) in DMF (6 ml) was heated for 22 hrs at 85⁰C. The resulting mixture was poured into ice-water mixture, stirred for 30 min. And the separated solid was purified by column chromatography to obtain two isomeric products in 18% and 12% yields respectively. Isomer A: M.P. 234-237⁰C; MS(M+1)- 422 ; M.F. C₁₈H₂₁F₂N₇O₃ Isomer B: M.P. 214-217⁰C; MS(M+1)- 422 ; M.F. C₁₈H₂JF₂N₇O₃

WOCKHARDT LIMITED [IN/IN]; D-4, MIDC Area, Chikalthana, Aurangabad 431006 (IN)

Our New Drug Discovery team has developed a number of lead molecules, mainly in the area of anti-infectives; these are currently at various stages of development.

Of these molecules, the most advanced of the New Chemical Entities (NCE) is WCK 771, which has commenced Phase II human clinical trials.

WCK 771 is a broad-spectrum antibiotic, which has proven effective in treating diverse staphylococcal infections like MRSA and VISA.

Other lead molecules at various stages of pre-clinical trials are: WCK 2349, WCK 4873 and WCK 4086.

http://www.wockhardt.com/how-we-touch-lives/new-drug-discover.aspx

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