C - Chemistry – Metallurgy – 12 – P
Patent
C - Chemistry, Metallurgy
12
P
C12P 13/04 (2006.01) C07C 323/59 (2006.01) C07C 323/63 (2006.01) C07D 285/36 (2006.01) C12P 11/00 (2006.01) C12P 41/00 (2006.01)
Patent
CA 2461296
The compounds of formula (I) are useful for the preparation of 1,5- benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1.beta.-converting enzyme, elastase or angiotensin enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor). The present invention relates to a new process for the preparation compounds of formula (I), wherein R1, R2, R3 and n are as described in the description which process comprises reacting compounds of formula (II), wherein R1, R2, R3, n and R4 are as described in the description, with a protease in an aqueous system containing an organic co-solvent.
Les composés de la formule (I) sont utiles dans la préparation de 1,5-benzothiazépines qui sont utiles en tant qu'inhibiteurs d'enzyme, tels que la protéase, l'enzyme de conversion d'interleukine-1.beta., l'enzyme de conversion d'élastase ou d'angiotensine, des antagonistes de GPCR (cholécystokinine, récepteur d'angiotensine II). La présente invention concerne un nouveau procédé de préparation de composés de la formule (I) dans laquelle R?1¿, R?2¿, R?3¿ et n ont la notation figurant dans la description, lequel procédé consiste à faire réagir des composés de la formule (II) dans laquelle R?1¿, R?2¿, R?3¿, n et R?4¿ ont la notation figurant dans la description, avec une protéase dans un système aqueux contenant un cosolvant organique.
Bleicher Konrad
Borthwick Scott
Iding Hans
Rogers-Evans Mark
Schmid Stefan
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
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