[EN] PROCESS FOR THE PREPARATION OF BIMATOPROST<br/>[FR] PROCÉDÉ DE PRÉPARATION DE BIMATOPROST
申请人:GENTEC S A
公开号:WO2017182465A1
公开(公告)日:2017-10-26
It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R1 is selected from (C1-C16)alkyl, (C1C16)haloalkyl, (C2-C16)alkenyl, (C2-C16)haloalkenyl, (C1-C16)alkoxy(C1-C16)alkyl, aryl, (C1-C16)alkylaryl, allyl, - (CH2-CH2-O)n-CH3 wherein n = 1, 2, 3 or 4, and -CH(O-CH2-CH2)2; R2 is selected from H, (C1-C16)alkyl, (C1-C16)haloalkyl, (C2-C16)alkenyl, (C2- C16)haloalkenyl, (C1-C16)alkoxy(CrC16)alkyl, aryl, (C1-C16)alkylaryl, allyl; or, alternatively, R1 and R2 taken together are selected from -CH2-CH2-CH2-, -CH2-CH2-, -O-CH2-CH2-, and -O-CH=CH-. There are also provided intermediates useful in such preparation process.
提供了一种制备比马前列素的方法,包括:a)在适当的溶剂存在下,将化合物(III)与乙胺发生反应;b)去保护步骤a)中得到的化合物,以获得比马前列素,其中R1选自(C1-C16)烷基,(C1-C16)卤代烷基,(C2-C16)烯基,(C2-C16)卤代烯基,(C1-C16)烷氧基(C1-C16)烷基,芳基,(C1-C16)烷基芳基,烯丙基,-(CH2-CH2-O)n-CH3其中n = 1, 2, 3或4,和-CH(O-CH2-CH2)2;R2选自H,(C1-C16)烷基,(C1-C16)卤代烷基,(C2-C16)烯基,(C2-C16)卤代烯基,(C1-C16)烷氧基(C1-C16)烷基,芳基,(C1-C16)烷基芳基,烯丙基;或者,R1和R2一起选自-CH2-CH2-CH2-,-CH2-CH2-,-O-CH2-CH2-,和-O-CH=CH-。还提供了在这种制备过程中有用的中间体。