申请人:American Cyanamid Company
公开号:US20020004600A1
公开(公告)日:2002-01-10
The invention relates to a process for the preparation of substituted pyrimidines of formula I,
1
wherein
R
1
, R
2
, R
3
, R
4
and X are as defined in claim
1,
which comprises reacting an amidine of formula II,
2
or a salt thereof, with a
3,3
—disubstituted vinylcarbonyl compound of formula III
3
wherein L represent a halogen atom or a group of formula —X—R
2
,
(a) in an inert solvent, in the presence of a base and a compound of formula IV
H—X—R
2
(IV)
in the event that L represent a halogen atom, or
(b) in an inert solvent and in the presence of a base, in the event that L represents a group of formula —X—R
2
.
本发明涉及一种制备式I,其中R1、R2、R3、R4和X如权利要求1所定义的取代嘧啶的方法,包括将式II的脲类化合物或其盐与式III的3,3-二取代乙烯酰基化合物反应,其中L代表卤素原子或式-X-R2的基团,在惰性溶剂中,在碱和式IV的化合物H-X-R2(IV)的存在下进行反应,当L代表卤素原子时,或在惰性溶剂中,在碱的存在下进行反应,当L代表式-X-R2的基团时。