发明名称 Process for the preparation of sildenafil and intermediates thereof
摘要 The present invention discloses a process for preparing sildenafil and its intermediates having the structures outlined below: In particular, the present invention provides a process for preparing the compound of formula (I) and its intermediates, i.e. the compounds of formula (I), (II), (III) and (IV). The compound of formula (I) is obtained from the compound of formula (II); the compound (II) is obtained from the compound of formula (III) and methylpiperazine; the compound (III) is obtained by treating the compound of formula (IV) with chlorosulfonic acid; the compound (IV) is obtained though treating the compound of formula (V) in the presence of at least one selected from POX3, PX3, PX5 and their mixtures in any ratio. The process for preparing the compound of formula (I) according to the present invention reduces the side reactions in the processes of the prior art. These improvements lead to higher yields and a better industrial applicability with easier controlling of the reaction.
申请公布号 US8071765(B2) 申请公布日期 2011.12.06
申请号 US20090448425 申请日期 2009.06.19
申请人 TIAN GUANGHUI;ZHU YI;LIU ZHENG;WANG ZHEN;SHEN JINGSHAN;TOPHARMAN SHANGHAI CO., LTD. 发明人 TIAN GUANGHUI;ZHU YI;LIU ZHENG;WANG ZHEN;SHEN JINGSHAN
分类号 C07D487/00 主分类号 C07D487/00
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