308847-79-2Relevant articles and documents
Vinylating of pyrimidine derivatives
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, (2008/06/13)
The invention relates to a process for the preparation of vinyl pyrimidines of the formula I wherein R1is hydrogen or a carboxylic ester group, and R2is hydrogen or a group of the formula (a) wherein Rais hydrogen, a protecting group or a group easily hydrolyzable under physiological conditions, by reacting a compound of the formula II wherein R21is hydrogen or a group (a) wherein hydroxy groups are optionally protected, R3is bromo, chloro or iodo, and R1is 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 R2is hydrogen with a compound of the formula IV wherein Rbis a hydroxy protecting group and Z is a leaving group, in the presence of a Lewis acid catalyst.