Method for preparing linezolid intermediate
AssigneesZhejiang Hisun Pharamceutical Co., Ltd., Shanghai Institute of Pharmaceutical Industry
InventorsFuli Zhang, Chunbo Yang, Bin Liang, Pengcheng Qiu, Hairong Luo, Jiang Li, Jian Chai, Qingfeng Cai
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Abstract
Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.
Claims9
A process for preparing an intermediate of Linezolid of Formula (I):
- the process comprises the following steps:
- a cyclization reaction of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III) is performed to obtain the compound of Formula (I),
- wherein R is a protected amino group as follows:
A process for preparing linezolid, wherein linezolid is prepared from the intermediate of Formula (I)
- wherein the intermediate of Formula (I) is prepared by the reaction as follows:
- a cyclization reaction of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III) is performed to obtain the compound of Formula (I), wherein R is a protected amino group as follows:
- followed by deprotection and acetylation to obtain linezolid.
Dependencies are inferred from the claim text.