| 摘要 |
1,205,085. Triazolylpyrazines. MERCK & CO. Inc. 11 Nov., 1968 [14 Nov., 1967], No. 53323/68. Heading C2C. The invention comprises compounds of formula and their pharmaceutically acceptable salts, wherein R<SP>1</SP> (in the 2- or 4-position) is H, C 1-5 alkyl or Ph-C 1-5 alkyl; R<SP>2</SP> is H, C 3-5 alkenyl, C 1-5 alkyl (possibly HO- or Ph substituted), amino or Ph; R<SP>3</SP> is H, C 1-5 alkyl or C 3-5 alkenyl; or R<SP>2</SP>R<SP>3</SP> may be -(CH 2 ) 4 -, -(CH 2 ) 5 - or (-CH 2 CH 2 ) 2 O; X is H or halogen; and Y is H, CF 3 , (CH 2 ) 4-7 N- or amino (possibly substituted, as defined in the Specification). These compounds are prepared by heating at 50-300‹ C. a compound of formula in which Z is 3-amino-5-Y-6-X-pyrazinyl, one R‹ is R<SP>1</SP> and the other is H. Starting materials and intermediates.-Details are given for the preparation of 1-methyl-1-(3,5- diamino - 6 - chloropyrazinoyl) hydrazine, 1- (benzylforamino) guanidine and its hydrochloride, 1 - (phenethylamino) guanidine hydrochloride, 1 - (3,5 - diamino - 6 - chloropyrazinoyl)- 3 - tert. - butylguanidine and 1 - (3,5 - diamino- 6-chloropyrazinoyl)-3,3-dibutylguanidine. Therapeutic compositions, for administration orally or by injection, comprise compounds of the above formula, which are diuretic and saluretic agents, together with an inert diluent, carrier or coating.
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