发明名称 |
PROCESS FOR PREPARING TORISEL |
摘要 |
A process for preparing Torisel, which is a derivative of Rapamycin, is provided. The process comprises the following steps: acetalating 2,2-dihydroxymethylpropionic acid with substituted or unsubstituted aromatic aldehyde in the presence of p-toluenesulfonic acid as catalyst to form the intermediate II; reacting the obtained intermediate with 2,4,6-trichlorobenzoyl chloride; then esterifying the obtained chloride with Rapamycin and finally deprotecting the diol to provide the product Torisel with yield over 35.6%. The aromatic aldehyde is one selected from benzaldehyde, p-methoxybenzaldehyde, p-chlorobenzaldehyde and p-trifluoromethyl benzaldehyde. |
申请公布号 |
EP2662376(B1) |
申请公布日期 |
2016.11.30 |
申请号 |
EP20110855154 |
申请日期 |
2011.05.16 |
申请人 |
TIANJIN WEIJIE TECHNOLOGY CO., LTD. |
发明人 |
SONG, HONGHAI;TANG, LONG;CHEN, WEI;LI, ZHENG;LI, JINZHOU;SUN, ZHICUN;FENG, JIAJIN |
分类号 |
C07D498/18 |
主分类号 |
C07D498/18 |
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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