Methods for preparing oxazolidinones and compositions containing them

Patent metadata

Field	Value
Publication number	US-9328087-B2
Application number	US-201314089050-A
Country	US
Kind code	B2
Filing date	Nov 25, 2013
Priority date	Oct 10, 2008
Publication date	May 3, 2016
Grant date	May 3, 2016

Abstract

Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.

First claim

What is claimed is:

1. A compound of the formula:

wherein:
R 1 a and R 1 b are independently selected from H and F, provided that at least one of R 1 a and R 1 b is F,
R 2 is selected from the group consisting of optionally substituted benzyl and optionally substituted C 1 -C 6 alkyl, and
Het is tetrazolyl optionally substituted with methyl.

2. The compound of claim 1 wherein R 1 a is F and R 1 b is H.

3. The compound of claim 1 wherein Het is substituted with methyl.

4. The compound of claim 3 wherein Het is 2-methyl-tetrazol-5-yl.

5. The compound of claim 1 wherein R 2 is benzyl.

6. The compound of claim 1 wherein R 1 a is F, R 1 b is H, R 2 is benzyl, and Het is 2-methyl-tetrazol-5-yl.

7. The compound of claim 1 wherein the optionally substituted benzyl and the optionally substituted C 1 -C 6 alkyl are independently unsubstituted or substituted with halogen or C 1 -C 4 alkyloxy.

Assignees

• Merck Sharp & Dohme

Inventors

• Costello Carrie A
• Ware Jacqueline A
• Duguid Robert J

Classifications

• A61P31/04

  Antibacterial agents · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• C07D403/10

  linked by a carbon chain containing aromatic rings · CPC title

• C07D413/14 Primary

  containing three or more hetero rings · CPC title

• C07F9/65583

  each of the hetero rings containing nitrogen as ring hetero atom · CPC title