申请人:Tobler Hans
公开号:US20120065239A1
公开(公告)日:2012-03-15
The present invention relates to a process for the preparation of compounds of formula I
wherein R
1
and R
2
are each independently of the other hydrogen or C
1
-C
5
alkyl and R
3
is CF
3
or CF
2
H, by
a) reaction of a compound of formula II
wherein R
1
and R
2
are as defined for formula I, with at least one reducing agent to form a compound of formula
wherein R
1
and R
2
are as defined for formula I, and
b) reaction of that compound with at least one reducing agent to form a compound of formula IV
wherein R
1
and R
2
are as defined for formula I, and
(c) reaction of that compound with a compound of formula V
wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C
1
-C
6
alkoxy and R
3
is as defined for formula I, to form the compound of formula I;
and to novel intermediates for use in that process.
本发明涉及一种制备式I化合物的方法,其中R1和R2分别独立地为氢或C1-C5烷基,R3为CF3或CF2H,包括以下步骤:
a)将式II化合物与至少一种还原剂反应,形成式III化合物,其中R1和R2如式I所定义;
b)将该化合物与至少一种还原剂反应,形成式IV化合物,其中R1和R2如式I所定义;
c)将该化合物与式V化合物反应,其中Q为氯、氟、溴、碘、羟基或C1-C6烷氧基,R3如式I所定义,形成式I化合物;
本发明还涉及用于该过程的新型中间体。