申请人:BEECHAM GROUP PLC
公开号:EP0009302A1
公开(公告)日:1980-04-02
The present invention provides a process for the preparation of a compound of the formula (I):
wherein R1 is a hydrogen atom, an alkyl group of up to 5 carbon atoms, a cycloalkyl group of 5 or 6 carbon atoms, a hydroxyalkyl group of up to 5 carbon atoms or a moiety of the sub formula (a):
wherein R2 is a hydrogen, fluorine, chlorine or bromine atom or an alkyl group of 1-3 carbon atoms, an alkoxyl group of 1-3 carbon atoms, an acyloxyl group of 1-3 atoms, a hydroxyl group, an alkoxycarbonyl group containing 1-3 carbon atoms in the alkoxy part, or a group -N(Rs)CO . R6, -N(R5)SO2R6 or -CO-NRsR6 where R5 is a hydrogen atom or an alkyl group of 1-3 carbon atoms or a phenyl or benzyl group and R6 is an alkyl group of 1-3 carbon atoms or a phenyl or benzyl group: R3 is a hydrogen, fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms, an alkoxyl group of 1-3 carbon atoms or an acyloxyl group of 1-3 carbon atoms; and R4 is a hydrogen fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms or an alkoxyl group of 1-3 carbon atoms. The disclosed process comprises inter alia the hydrogenation of a compound of the formula (II):
or a hydrogenolysable ester thereof wherein R1 is as defined in relation to formula (I) or R1 is R'1 a moiety that on hydrogenation provides a group R1 as defined in formula (I), R8 is a lower atom or a lower alkyl group and R10 is a hydrogen atom or a lower alkyl or phenyl group. The compounds of the formula (III) are useful intermediates and as such form part of this invention.
本发明提供了一种制备式(I)化合物的工艺:
其中 R1 是氢原子、最多 5 个碳原子的烷基、5 或 6 个碳原子的环烷基、最多 5 个碳原子的羟烷基或亚式(a)的分子:
其中 R2 是氢、氟、氯或溴原子或 1-3 个碳原子的烷基、1-3 个碳原子的烷氧基、1-3 个原子的酰氧基、羟基、烷氧基部分含有 1-3 个碳原子的烷氧羰基或基团 -N(Rs)CO .R6、-N(R5)SO2R6 或 -CO-NRsR6 其中 R5 是氢原子或 1-3 个碳原子的烷基或苯基或苄基,R6 是 1-3 个碳原子的烷基或苯基或苄基:R3是氢、氟或氯原子或1-3个碳原子的烷基、1-3个碳原子的烷氧基或1-3个碳原子的酰氧基;R4是氢氟或氯原子或1-3个碳原子的烷基或1-3个碳原子的烷氧基。所公开的工艺包括将式(II)化合物氢化:
或其可氢解酯,其中 R1 如式 (I) 所定义,或 R1 是 R'1 的分子,氢化后可得到如式 (I) 所定义的基团 R1,R8 是低级原子或低级烷基,R10 是氢原子或低级烷基或苯基。式(III)化合物是有用的中间体,因此构成本发明的一部分。