Synthesis and antitumor activity of 5-mercapto-9-ethoxycarbonyl-1, 2-dihydro-3h-pyrimido-[5, 4-e] pyrrolizine derivatives

AV Kadushkin, TV Golovko, SG Kalistratov…

Index: Kadushkin, A. V.; Golovko, T. V.; Kalistratov, S. G.; Sokolov, A. S.; Chernov, V. A.; Granik, V. G. Pharmaceutical Chemistry Journal, 1987 , vol. 21, # 5 p. 317 - 322 Khimiko-Farmatsevticheskii Zhurnal, 1987 , vol. 21, # 5 p. 545 - 550

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Abstract

It is generally known that a number of pyrrolo [3, 2-d] pyrimidine derivatives have been found to possess pronounced antitumor activity [2]. We have recently demonstrated that enamines obtained by reacting N-cyanomethylpyrrolid-2-one diethylacetal (I) with compounds containing an active methyl ring are easily cyclized by the Thrope--Ziegler method into derivatives of 5-cyano-6-aminopyrrolizidine [i]. The presence of cyano and amino groups ...