| 摘要 |
1,174,305. Biguanides. SANDOZ Ltd. 17 March, 1967 [13 April, 1966; 28 Dec., 1966], No. 12700/67. Heading C2C. Compounds of the general formula and their salts, wherein R is H or 1-4 C-alkyl are prepared either by heating a compound of the formula with a compound B-NH-R where one of A and B is H and the other is an N-cyanocarboxamidine radical in the presence of at least one equivalent of an acid or (when R is H only) reacting compound II (A=H) with a pyrazole derivative of the formula wherein R 1 and R 2 are H, 1-4 C alkyl, aryl or aralkyl radicals, in a suitable solvent and in the presence of at least one equivalent of acid. N<SP>1</SP> - leyano - 3 - azabicyclo[3,2,0] - heptane - 3- carboxamidine is prepared from 3-azabicyclo [3,2,0]heptane, HCI and Na dicyanimide and N - guanyl 1 - pyrazole - carboxamidine from 1 - pyrazole-carboxamidine and triethylamine. Pharmaceutical compositions comprise the compounds I and an inert carrier. The compounds which are useful as antidiabetic agents are administered orally in the usual forms.
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