发明名称 |
AN EFFICIENT PROCESS FOR SEPARATION OF DIASTEREOMERS OF 9-[(R)-2-[[(R,S)-[[(S)-1-(ISOPROPOXYCARBONYL)ETHYL]AMINO]-PHENOXYPHOSPHINYL] METHOXY]PROPYL]ADENINE |
摘要 |
The present invention relates to an efficient process for the separation of diastereomers of 9-[(R)-2-[[(R,S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]-phenoxyphosphinyl]methoxy]propyl]adenine and to a process for preparing 9-[(R)-2-[[(R)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine and 9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine. |
申请公布号 |
US2016122373(A1) |
申请公布日期 |
2016.05.05 |
申请号 |
US201414896313 |
申请日期 |
2014.06.06 |
申请人 |
CIPLA LIMITED |
发明人 |
RAO Dharmaraj Ramachandra;SAWANT Ashwini Amol;SHIVALKAR Nayan;THAKUR Nitin |
分类号 |
C07F9/6561 |
主分类号 |
C07F9/6561 |
代理机构 |
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代理人 |
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主权项 |
1. A process for preparing 9-[(R)-2-[[(R)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine or 9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine, comprising one or more of the following steps (a-c):
a. reacting phenyl((R)-1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl phosphonochloridate with 2-amino-propionic acid isopropyl ester or the hydrochloride salt thereof and a suitable chiral organic acid to obtain a diastereomeric organic acid addition salt of 9-[(R)-2-[[(R,S)-[[(S)-1(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine; and/or b. crystallising a diastereomeric organic acid addition salt of 9-[(R)-2-[[(R,S)-[[(S)-1(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine using a suitable solvent or mixture of solvents; and/or c. treating a diastereomeric organic acid addition salt of 9-[(R)-2-[[(R,S)-[[(S)-1(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine with a suitable base; and optionally thereafter performing one or more of the following steps: d. isolating 9-[(R)-2-[[(R)-[[(S)-1(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine or 9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine; and/or e. increasing the diastereomeric purity of the product so formed. |
地址 |
Mumbia IN |