A CONVENIENT SYNTHESIS OF (#ZETA#)-3-(#alpha#-CYANO-#alpha#-ALKOXY-CARBONYLMETHYLENE)-2-PIPERAZINONES AND THEIR DERIVATIVES

摘要

(#ZETA#)-3-(#alpha#-Cyano-#alpha#-alkoxycarbonylmethylene)-2-piperazinone derivatives (3) and trans-(#ZETA#)-3-(#alpha#-cyano-#alpha#-alkoxycarbonylmethylene)-octahydro-2(1H)-quinoxalinone drivatives (5) possessing various alkoxycarbonyl groups are prepared directly from the reaction of dialkyl (E)-2,3-dicyanobutenedioates (1) with ethylenediamine (2) and with trans-1,2-diaminocyclohexane (4),respectively.Furthermore,cis-1,2-diaminocycloheptane (6) and meso-2,3-diaminobutane (8) were reacted with the diethyl ester 1b to give cis-(#ZETA#)-3-(#alpha#-cyano-#alpha#-ethoxycarbonyl-methylene)decahydro-2H-cycloheptapyrazin-2-one (7) and cis-(3ZETA#)-3-(3alpha#-cyano-#alpha#-ethoxycarbonylmethylene)-5,6-dimethyl-2-piperazinone (9),respectively.The structural studies of3,5,7,and 9were carried out by NMR experiments in some details;.