Process for the preparation of vinyl pyrimidine derivatives

Details Process for the preparation of vinyl pyrimidine derivatives Process for the preparation of vinyl pyrimidine derivatives

C - Chemistry, Metallurgy

07

H

C07H 19/06 (2006.01) C07D 239/47 (2006.01)

Patent

CA 2309111

The invention relates to a process for the preparation of vinyl pyrimidines of the formula I Image wherein R1 is hydrogen or a carboxylic ester group, and R2 is hydrogen or a group of the formula (a) Image wherein R a is hydrogen, a protecting group or a group easily hydrolyzable under physiological conditions, by reacting a compound of the formula II Image wherein R21 is hydrogen or a group (a) wherein hydroxy groups are optionally protected, R3 is bromo, chloro or iodo, and R1 is as above, with a vinyl borane compound in the presence of a Pd complex and a base, and optionally, further reacting a product of formula I wherein R2 is hydrogen with a compound of the formula IV Image wherein R b is a hydroxy protecting group and Z is a leaving group, in the presence of a Lewis acid catalyst.

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