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 2727674

The present invention relates to methods of making compounds that inhibit 11- .beta.-hydroxysteroid dehydrogenase type 1 enzyme (11-.beta. HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, 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 préparation de composés qui inhibent lenzyme 11-ß-hydroxystéroïde déshydrogénase de type 1 (11-ß HSD1). Un procédé comprend (a) la mise en contact dun composé de formule (II) avec une base chirale, un agent de déprotonation, et un agent dalkylation R3-LG, (b) la mise en contact du produit de (a) avec un acide pour former un sel, et (c) la réaction du sel avec une base pour former le composé de formule (I) ; où Z, R1, R2, et R3 sont présentement définis.

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