申请人:American Cyanamid Company
公开号:US06281358B1
公开(公告)日:2001-08-28
The invention relates to a process for the preparation of substituted pyrimidines of formula I,
wherein
R1, R2, R3, R4 and X are as defined in claim 1, which comprises reacting an amidine of formula II,
or a salt thereof, with a 3,3-disubstituted vinylcarbonyl compound of formula III
wherein L represent a halogen atom or a group of formula —X—R2,
(a) in an inert solvent, in the presence of a base and a compound of formula IV
H—X—R2 (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—R2.
该发明涉及一种制备式I的取代嘧啶化合物的方法,
其中
R1、R2、R3、R4和X如权利要求1所定义,包括将式II的酰胺
或其盐与式III的3,3-二取代乙烯羰基化合物反应,
其中L代表卤素原子或式—X—R2的基团,
(a)在惰性溶剂中,在碱和式IV的化合物的存在下
H—X—R2 (IV)
如果L代表卤素原子,或
(b)在惰性溶剂中,在碱的存在下,如果L代表式—X—R2的基团。