Invention Grant
US08507716B2 Process for preparing pemetrexed disodium and its intermediate, 4-(4-carbomethoxyphenyl) butanal
失效
制备培美曲塞二钠及其中间体4-(4-甲酯基苯基)丁醛的方法
- Patent Title: Process for preparing pemetrexed disodium and its intermediate, 4-(4-carbomethoxyphenyl) butanal
- Patent Title (中): 制备培美曲塞二钠及其中间体4-(4-甲酯基苯基)丁醛的方法
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Application No.: US12995257Application Date: 2008-11-25
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Publication No.: US08507716B2Publication Date: 2013-08-13
- Inventor: Jinliang Li , Nan Zhao
- Applicant: Jinliang Li , Nan Zhao
- Applicant Address: CN Shanghai
- Assignee: Shanghai Cdymax Pharmaceuticals Co., Ltd
- Current Assignee: Shanghai Cdymax Pharmaceuticals Co., Ltd
- Current Assignee Address: CN Shanghai
- Agency: Fish & Richardson P.C.
- Priority: CN200810038375 20080530
- International Application: PCT/CN2008/073182 WO 20081125
- International Announcement: WO2009/143684 WO 20091203
- Main IPC: C07C69/76
- IPC: C07C69/76 ; C07C69/95

Abstract:
The present invention provides a process for preparing pemetrexed disodium and its intermediate, 4-(4-carbomethoxyphenyl)butanal. The process for preparing the intermediate comprises the following steps: condensing methyl 4-bromobenzoate with 3-buten-1-ol; extracting with an organic solvent during the work-up; adding silica gel to decolorize; and evaporating the organic solvent to give 4-(4-carbomethoxyphenyl)butanal. The product obtained by the present process, with a yield of higher than 80%, and a purity measured by GC of higher than 95%, may be directly used in the next bromination reaction for synthesizing pemetrexed disodium without purification. The present process is suitable for industrial production, as the operation is simple and the reagents used are cheap and readily available.
Public/Granted literature
- US20110124861A1 Process for Preparing Pemetrexed Disodium and Its Intermediate, 4-(4-Carbomethoxyphenyl) Butanal Public/Granted day:2011-05-26
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