发明名称 |
PROCESS FOR PRODUCING 2-AMINO-2-[2-[4-(3-BENZYLOXYPHENYLTHIO)-2-CHLOROPHENYL[ETHYL]-1,3-PROPANEDIOL HYDROCHLORIDE AND HYDRATES THEREOF. AND INTERMEDIATES THE PRODUCTION THEREOF |
摘要 |
<p>A process for the industrial production of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (Compound I), an effective immunosuppressant. The process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride or a hydrate thereof includes the steps of reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to form ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate; reducing the resulting ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, followed by mesylation, iodination and nitration, to form 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene; forming 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol using a formaldehyde solution; and reducing the resulting 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol to form the desired product.</p> |
申请公布号 |
EP1806338(B1) |
申请公布日期 |
2016.01.20 |
申请号 |
EP20050790615 |
申请日期 |
2005.10.07 |
申请人 |
KYORIN PHARMACEUTICAL CO., LTD. |
发明人 |
TSUBUKI, TAKESHI;KOBAYASHI, KENICHI;KOMATSU, HIDETAKA |
分类号 |
C07C319/20;A61K31/137;A61P1/04;A61P11/06;A61P13/12;A61P17/00;A61P19/02;A61P29/00;A61P37/06;A61P37/08;C07C319/12;C07C323/07;C07C323/32;C07C323/56 |
主分类号 |
C07C319/20 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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