The present invention relates to a new process for the preparation compounds of formula I
1
wherein R
1
, R
2
, R
3
and n are as described in the description which process comprises
reacting compounds of formula II
2
wherein R
1
, R
2
, R
3
, n and R
4
are as described in the description,
with a protease in an aqueous system containing an organic co-solvent.
The compound of formula I are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1&bgr;-converting enzyme, elastase or angiotensin converting enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor).
本发明涉及一种制备式I1化合物的新工艺,其中R1、R2、R3和n如描述中所述,该工艺包括将式II2化合物与
蛋白酶在含有有机共溶剂的
水系中反应。式I的化合物可用于制备1,5-
苯并噻吩,其可用作酶
抑制剂,如
蛋白酶、白细胞介素-1β
转化酶、
弹性蛋白酶或
血管紧张素转化酶、
GPCR拮抗剂(胆囊收缩素、
血管紧张素II受体)。