申请人:Technopharma S.A.
公开号:EP1721894A1
公开(公告)日:2006-11-15
An alternative method for the synthesis of prostaglandin F analogues, in particular, analogues of PGF2α and specifically for the synthesis of latano-prost, wherein the transformation of the lactone intermediate (5)
into the corresponding lactol (7)
is carried out by treating the lactone intermediate (5) with a silane, preferably polymethylhydrosiloxane (PMHS), in the presence of a titanocene - and preferably titanocene fluoride.
The method enables considerable production economies with respect to the conventional reduction of lactone with diisobutylaluminum hydride (DIBAL-H).
一种合成前列腺素F类似物的方法,特别是PGF2α类似物,特别是用于合成拉坦前列腺素,其中通过用硅烷处理乳内中间体(5),优选使用聚甲基氢硅氧烷(PMHS),在存在钛烯化合物,最好是钛烯氟化物的情况下,将乳内中间体(5)转化为相应的乳糖(7)。
该工艺与二异丁基氢化铝(DIBAL-H)还原内酯相比,可显著降低生产成本。