Process for preparing linezolid

C - Chemistry – Metallurgy – 07 – D

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C07D 413/10 (2006.01) C07C 251/06 (2006.01)

Patent

CA 2648178

The present invention relates to a new process for preparing the oxazolidinone antibacterial agent linezolid which comprises the reaction of an (S)-I -chloro-3- (benzyIidenylamino)-propan-2-ol with a morpholinyl fluorophenyl carbamate to afford a protected imine intermediate which, upon hydrolysis and acylation, yields linezolid in high yield.

La présente invention concerne un nouveau procédé de préparation du linézolide, un agent antibactérien oxazolidinone, ledit procédé impliquant de faire réagir un (S)-I-chloro-3- (benzylidénylamino)propan-2-ol avec un morpholinyle fluorophényle carbamate afin d'obtenir un intermédiaire imine protégé, lequel conduit par hydrolyse et acylation au linézolide, avec un rendement élevé.

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