methods for the microbiological transformation of benzodiazepineverbindingen.

摘要

1374492 Benzodiazepines SUMITOMO CHEMICAL CO Ltd 19 June 1972 [18 June 1971] 28690/72 Heading C2C Compounds of the general formula (R 1 =H, carbamoyl, C 1 -C 4 alkyl-carbamoyl, C 1 -C 4 alkyl, C 3 -C 6 cycloalkyl, C 2 -C 5 alkenyl, C 3 -C 5 alkynyl, the alkyl, alkenyl or alkynyl group being optionally substituted by 1-3 radicals selected from halogen, C 3 -C 6 cycloalkyl, aryl, heterocyclic, aralkyl, acyl, carbamoyl, C 1 -C 4 alkylcarbamoyl, amino, C 1 -C 4 alkylamino, di(C 1 -C 4 alkyl)amino, XR 6 ; X = O, S, SO 2 , SO; R 6 =H, C 1 -C 4 alkyl or haloalkyl, C 1 -C 4 alkoxy-C 1 -C 4 alkyl, C 2 -C 5 alkenyl, C 3 -C 5 alkynyl, aryl, acyl, aralkyl, heterocyclic, carbamoyl, C 1 -C 4 alkylcarbamoyl; R 2 = H, halogen, C 1 -C 4 alkyl R 3 =H, halogen, C 1 -C 4 alkyl or alkoxy; R 4 = halogen, CF 3 , C 1 -C 4 alkyl or alkoxy, NO 2 ; R 5 = H, halogen, C 1 -C 4 alkyl or alkoxy; n=0, 1), are prepared by fermenting a compound of the formula in the presence of a strain of Streptomyces which has a hydroxylating enzyme system, or incubating it with resting cells previously grown in a culture medium. Removal of a 1-substituent may also occur.