Selective synthesis of cf3-substituted pyrimidines

Details Selective synthesis of cf3-substituted pyrimidines Selective synthesis of cf3-substituted pyrimidines

C - Chemistry, Metallurgy

07

D

C07D 239/42 (2006.01)

Patent

CA 2537373

The present invention relates to a method of making a compound of the formula (I),wherein X1, X2 and R3-R4 are as defined herein. The method includes reacting a compound of the formula (II) with an amine of formula (III) (HNR3R4) in the presence of a Lewis Acid and a non-nucleophilic base. The 2,4- diamino pyrimidine moiety is a common component in a variety of biologically active drug-like molecules and pyrimidine derivatives have been found to be useful in the 10 treatment of abnormal cell growth, such as cancer, in mammals.

La présente invention concerne un procédé pour fabriquer un composé de la formule (I) dans laquelle X?1¿, X?2 ¿et R?3¿-R?4¿ sont tels que définis dans le présent fascicule. Ce procédé consiste à faire réagir un composé de la formule (II) avec une amine de formule (III) (HNR?3¿R?4¿) en présence d'un acide de Lewis et d'une base non nucléophile. La fraction 2,4-diamino pyrimidine est un constituant courant dans une grande variété de molécules médicamenteuses biologiquement actives, et des dérivés pyrimidiques se sont révélés utiles dans le traitement de la croissance cellulaire anormale, telle que le cancer, chez les mammifères.

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