| 摘要 |
<p>The invention comprises pregnane-20-guanylhydrazones having at the 3-position a halogen atom or an alkyl, alkynyl, aryl, alkoxy, cycloalkoxy, carboxy, carbalkoxy, cyano, acylamino, oxime, hydrazone, semicarbazone, thiosemicarbazone, urea, thiourea, N1-alkylthiourea or phosphoric acid ester group or, in 3,5-cyclocompounds, a b -hydrogen atom, or containing at the 2,3-position a fused pyrazole, N-carbamylpyrazole, isoxazole, thiazole, pyrrole, thiazole or oxirane ring, and their preparation by (1) reaction of a 20-keto-pregnane with (a) aminoguanidine or an acid addition salt thereof, (b) thiosemicarbazide, O- or S-alkyl-iso-thiosemicarbazide, or an acid addition salt thereof, with optional conversion of a thiosemicarbazone to an S-alkyl-isothiosemicarbazone, and subsequently ammonia, or (c) hydrazine and subsequently cyanamide, or (2) reaction of a 3-keto-pregnane-20-guanylhydrazone with semicarbazide, thiosemicarbazide, hydrazine hydrate or hydroxylamine hydrochloride. The compounds of the invention have cardiotonic activity. 3b - Acetylamino - pregnan - 20 - one is prepared by acetylation of the free amine with acetic anhydride. N - Methyl - N1 - (pregnan - 20 - one - 3b - yl) thiourea is prepared by reaction of 3b -amino-pregnan-20-one with methyl isothiocyanate. Pregnenolone-3-phosphate is prepared by reaction of pregnenolone with phosphorus oxychloride.</p> |
