| 摘要 |
1471629 Amidine derivatives UPJOHN CO 5 Feb 1975 [11 Feb 1974] 4826/75 Heading C2C Compounds of formula wherein R 1 is cycloalkyl of 5 to 8 carbon atoms, adamantyl, phenyl, mono- or di-substituted phenyl or phenalkyl or mono- or di-ring substituted phenalkyl wherein the alkyl part contains 1 to 3 carbon atoms and each substituent is selected from alkyl and alkoxy of 1 to 3 carbon atoms, halogen and trifluoromethyl; R 2 is alkyl of 1 to 8 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, adamantyl, phenyl or phenalkyl wherein the alkyl part contains 1 to 3 carbon atoms; R 3 and R 4 are each selected from alkyl of 1 to 6 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, phenyl, mono-substituted phenyl or phenalkyl or mono-ring substituted phenalkyl wherein the alkyl part contains 1 to 3 carbon atoms and each substituent is selected from alkyl and alkoxy of 1 to 3 carbon atoms, halogen and trifluoromethyl, or NR 3 R 4 is morpholino, thiomorpholino, pyrrolidino, piperidino, perhydroazepino, piperazino or N-alkylpiperazino wherein the alkyl group is of 1 to 3 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof are prepared from the corresponding amide (R 1 CONHR 2 ) and amine (R 3 NHR 4 ). Amides R 1 CONHR 2 (R 1 = cyclohexyl or pchlorophenyl; R 2 = cyclohexyl) are prepared by reaction of R 1 COCl with R 2 NH 2 .
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