申请人:KANEKA CORPORATION
公开号:EP1074544A1
公开(公告)日:2001-02-07
The present invention has for its object to provide a process for producing a 3-(3-pyridyl)-1-propanol derivative of use as a pharmaceutical intermediate expediently with an inexpensive material.
The present invention provides a process for producing a 3-(3-pyridyl)-1-propanol derivative (3):
in the formula, R1 represents an alkyl group of 1 to 20 carbon atoms, aryl group of 6 to 20 carbon atoms or aralkyl group of 7 to 20 carbon atoms, which may be substituted,
which comprises reacting a 3-methylpyridine with a strong base to prepare a 3-methylpyridine metal (1):
in the formula, M represents lithium, sodium, potassium or a magnesium halide, where the halide is chloride or bromide,
and then reacting said metal salt with an epoxy compound (2):
本发明的目的是提供一种用廉价材料快速生产用作药物中间体的 3-(3-吡啶基)-1-丙醇衍生物的工艺。
本发明提供了一种生产 3-(3-吡啶基)-1-丙醇衍生物(3)的工艺:
式中,R1 代表 1 至 20 个碳原子的烷基、6 至 20 个碳原子的芳基或 7 至 20 个碳原子的芳烷基,可被取代、
其中包括将 3-甲基吡啶与强碱反应,制备 3-甲基吡啶金属 (1):
式中,M 代表锂、钠、钾或卤化镁,其中卤化物为氯化物或溴化物、
然后将所述金属盐与环氧化合物(2)反应: