申请人:Zaklady Farmaceutyczne "Polpharma" S.A.
公开号:EP3725774A1
公开(公告)日:2020-10-21
This invention relates to a process for the preparation of pimavanserin comprising: (i) providing an acid addition salt of pimavanserin; (ii) dissolving the acid addition salt of pimavanserin in an aqueous solvent to form an aqueous solution; (iii) washing the aqueous solution obtained in step (ii) with an organic solvent; and (iv) adding a base to the washed aqueous solution to form pimavanserin. The invention also relates to a process for the preparation of an acid addition salt of pimavanserin additionally comprising step (v) of converting pimavanserin into an acid addition salt of pimavanserin.
The invention also relates to pimavanserin or an acid addition salt thereof obtainable by the process, and to the use of pimavanserin hydrochloride, pimavanserin hydrogen sulfate or pimavanserin acetate for preparing pimavanserin or an acid addition salt thereof.
本发明涉及一种制备pimavanserin的工艺,包括:(i)提供pimavanserin的酸加成盐;(ii)将pimavanserin的酸加成盐溶解在水性溶剂中形成水溶液;(iii)用有机溶剂洗涤步骤(ii)中得到的水溶液;以及(iv)向洗涤后的水溶液中加入碱形成pimavanserin。本发明还涉及一种制备匹马色林的酸加成盐的工艺,该工艺还包括将匹马色林转化为匹马色林的酸加成盐的步骤(v)。
本发明还涉及可通过该工艺获得的匹马伐林或其酸加成盐,以及使用盐酸匹马伐林、硫酸氢匹马伐林或醋酸匹马伐林制备匹马伐林或其酸加成盐。