| 摘要 |
1,265,764. Mandelamidines. ORSYMONDE. 20 April, 1970 [23 April, 1969], No. 18696/70. Addition to 1,243,186. Heading C2C. Novel mandelamidines of the general formula wherein R 1 and R 2 are each a hydrogen atom or a hydroxy, C 1-3 alkyl or C 1-3 alkoxy group or together represent a C 1-3 alkylenedioxy group, R 3 is a hydrogen atom or a C 1-3 alkyl or phenyl group and R 4 is a hydroxy, C 2-3 alkyl or phenyl group or, when R 2 is a hydroxy or C 1-3 alkoxy group and R 1 is a hydrogen atom or when R 2 is a hydroxy group and R 1 is a C 1-3 alkoxy group or when R 1 and R2 are together a C 1-3 alkylenedioxy group, R 4 may be a hydrogen atom or methyl group, and non-toxic acid addition salts thereof are prepared (a) when R 4 is not a hydroxy group, by reaction of a mandelonitrile of the general formula with an aliphatic alcohol, followed by ammonia or an amine of the general formula NHR 3 R 4 ; and (b) when R 4 is a hydroxy group, by reaction of the corresponding mandelamidine of the first general formula above wherein R 4 is a hydrogen atom with hydroxylamine; followed optionally by salification of the product or resolution into its optically active forms. Pharmaceutical compositions, useful in the treatment of arterial hypertension, comprise, as active ingredient, at least one mandelamidine of the first general formula above or non-toxic acid addition salt thereof, together with a non- toxic pharmaceutical carrier. |
