摘要 |
6,7,8,9-Tetrahydropyrazolo[3,4-b][1,5]diazocine compounds (I; R1 is methyl or ethyl, R2 is methyl, ethyl or nitro, R3 is hydrogen, methyl, ethyl, nitro, trifluoroacetyl, dialkylaminoalkyl or 1-pyrrolidinylethyl, R4 and R5 are hydrogen or lower alkyl, R6 is hydrogen or methyl, Z is N or N->O, and Ar is phenyl, substituted phenyl, cyclohexyl, 2-thienyl or 2-pyridyl) are provided by several methods: (a) reacting a 4-(aroyl)-5-chloropyrazole with a 1,3-alkanediamine, (b) alkylating, (c) nitrating, or (d) trifluoroacetylating a pyrazolodiazocine at the N9-position, (e) forming the N5-oxide of a pyrazolodiazocine, and (f) hydrolyzing a 9-trifluoroacetylpyrazolodiazocine. The compounds are useful as intermediates and as antidepressant agents. |