Process for preparing aromatase inhibitors

Details Process for preparing aromatase inhibitors Process for preparing aromatase inhibitors

C - Chemistry, Metallurgy

07

J

C07J 1/00 (2006.01) A61K 31/565 (2006.01)

Patent

CA 2686312

A process of making an aromatase inhibitor of formula (I) : wherein each of R1, R2, R3, and R4, independently, is hydrogen, halogen, or C1-C6 alkyl, comprising reacting a compound of formula (II) : with an acid in the presence of a suitable solvent. A new crystalline form of exemestane and is also disclosed.

L'invention concerne un procédé de fabrication d'un inhibiteur de l'aromatase de formule (I) : dans laquelle formule chacun de R1, R2, R3 et R4 représente indépendamment un hydrogène, un halogène ou un alkyle en C1-C6, lequel procédé consiste à faire réagir un composé de formule (II) : avec un acide en présence d'un solvant approprié. L'invention concerne également une nouvelle forme cristalline de l'exémestane.

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