Process for making substituted 2-amino-thiazolones

Details Process for making substituted 2-amino-thiazolones Process for making substituted 2-amino-thiazolones

C - Chemistry, Metallurgy

07

D

C07D 277/54 (2006.01) C07D 263/48 (2006.01)

Patent

CA 2692128

The present invention relates to methods of making compounds that inhibit 11- - hydroxysteroid dehydrogenase type 1 enzyme (11- HSD1). One method comprises (a) contacting a compound of formula (II) sequentially with a chiral base in the presence of an amine, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I), wherein Z, R1, R2, and R3 are defined herein.

La présente invention concerne des procédés de fabrication de composés qui inhibent l'enzyme 11-bêta-hydroxystéroïde déshydrogénase de type 1 (11b-HSD1). L'un desdits procédés consiste à (a) mettre en contact un composé de formule (II) séquentiellement avec une base chirale en présence d'une amine et avec un agent alkylant R3-LG, (b) mettre en contact le produit de (a) avec un acide pour former un sel et (c) faire réagir le sel avec une base pour former le composé de formule (I). (Dans la formule, Z, R1, R2 et R3 sont tels que définis ici.)

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