The invention discloses a new method of synthesizing a 1, 2, 3-triazol 1, 3-diazacyclo compound with pharmaceutical activity. The structure of the 1, 2, 3-triazol 1, 3-diazacyclo compound with pharmaceutical activity is shown in figure (1), wherein n is equal to 1, 2 or 3; z is an O atom, an S atom or NR'; R' is a
hydrogen atom, methyl,
nitryl, cyano, amido, C[1-8]
alkyl, C[1-8]alkylamino, C[1-8]alkanoyl, aroyl, dense aroyl,
aryl, dense
aryl, naphthenic base, aralkyl, oxa-
alkyl, oxa-acyl, thia-
alkyl or thia- acyl; R is alkyl,
aryl, substituted aryl or heterocyclic aryl; n is equal to 1, 2 or 3; Z is an O atom, an S atom or NH preferably; and R is methyl, phenyl, p-methylphenyl, p-chlorphenyl or p-methoxyphenyl preferably. The invention is characterized in that, substituted
halobenzene, hydrazoates and heterocyclic
ketene amines or derivatives thereof are used for preparing the 1, 2, 3-triazol 1, 3-diazacyclo compound which has pharmaceutical activity and has the structure shown in figure (1) at high yield by the one kettle way. The invention has the advantages of simple synthesizing technology, moderate conditions and high yield. The invention achieves the synthesis of
heterocyclic compound libraries at high yield in a parallel mode by the one kettle way, and really achieves molecular multiformity. In addition, the invention has the characteristics of high yield, simple lines, moderate conditions and the like.