- Development of a pilot-scale preparation of N-[[(5S)-3-[4-(1,1-dioxido-4- thiomorpholinyl)-3,5-difluorophenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, PNU-288034, an oxazolidinone antibacterial agent
-
As part of Pfizer's continuing efforts in the oxazolidinone area, we have developed an efficient synthesis of PNU-288034 and successfully implemented it on pilot scale. The key step was a novel, acid-catalyzed, double Michael addition of 2,6-difluoroanili
- Lu, Cuong V.,Chen, Jiong J.,Perrault, William R.,Conway, Brian G.,Maloney, Mark T.,Wang, Ying
-
p. 272 - 277
(2012/12/22)
-
- Amide-containing compound having improved solubility and method of improving the solubility of an amide-containing compound
-
The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compounds and the bioavail
- -
-
-
- N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
-
The present invention provides antibacterial agents having the formulae I, II, and III described herein.
- -
-
-
- N-ARYL-2-OXAZOLIDINONE-5-CARBOXAMIDES AND THEIR DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
-
Compounds of formula B-C-A-CO-NH-R1, wherein A is structure i, ii or iii: formulae (I), (II), (III). C is optionally substituted aryl or heteroaryl, and B is a specified cyclic moiety, or C and B together are a heterobicyclic moiety, are useful as antibacterial agents.
- -
-
Page/Page column 91
(2010/02/07)
-
- Catalyzed double Michael addition of anilines to vinyl sulfone
-
Substituted anilines and vinyl sulfone undergo a facile double Michael addition to form substituted phenylthiomorpholine dioxide, catalyzed with AlCl3 or H3PO4. Scope and conditions were explored.
- Chen, Jiong Jack,Lu, Cuong V.,Brockman, Rebecca N.
-
p. 3459 - 3462
(2007/10/03)
-
- Method for the preparation of oxazolidinones
-
The present invention relates to a method for the production of N-({(5S)-3-[4-(1,1-dioxido-4-thiomorpholinyl)-3,5-difluorophenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide or its pharmaceutically acceptable salt.
- -
-
-