method получени  derivatives эрголена or эрголина

摘要

1,244,880. Ergolene derivatives. SANDOZ Ltd. 30 Dec., 1968 [18 Jan., 1968; 4 Nov., 1968], No. 61609/68. Heading C2C. Novel compounds I in which x-y is -CH 2 -CH or -CH=C, and R is C 7-9 aralkyl or aryl, either of which may be substituted by halo, C 1-4 alkyl, C 1-4 alkoxy, amino or acylamino, the acyl radical of which is derived from a C 2-5 aliphatic or an aromatic carboxylic acid are prepared by (a) reduction of compounds of the general Formula II in which RSP1/SP is as above with the exception of acylamino and the amino radical may be protected, with a selective carbonyl to methylene reducing agent or (b) catalytic hydrogenation of compounds I in which x-y is -CH=C and R is as defined above for RSP1/SP; splitting off any protective radical from the amino group and optionally acylating the resulting amino compounds. Intermediates isolated are the compounds of Formula II which are prepared from d-lysergic acid hydrochloride and the appropriate N- phenyl - piperazine derivative; 4 - (p - tritylaminophenyl) - piperazine, prepared from 1- carbethoxy - 4 - (p - tritylaminophenyl)piperazine which is prepared from 1 - carboethoxy - 4- (p - aminophenyl)piperazine and trityl chloride; d - lysergic acid N - (p - nitrophenyl) - piperazide, prepared from d-lysergic acid chloride and N - (p - nitrophenyl)piperazine and d - lysergic. acid N - (p - aminophenyl)piperazide, prepared from the previous intermediate by reduction. Pharmaceutical compositions for oral, rectal or parenteral application comprise a compound I in admixture with a suitable pharmaceutical excipient and are used as antidepressants, antihypertensives and sedatives.