Abstract An efficient synthesis of 4-chloro-2-pyrrolino [2, 3-d] pyrimidin-6-one was achieved in four steps starting from dimethyl malonate in 23% overall yield. This synthesis was demonstrated on 100 g scale to obtain 4-chloro-2-pyrrolino [2, 3-d] pyrimidin-6-one in 98.5% purity. Similarly, 7-[(2, 4-dimethoxyphenyl) methyl]-4-chloro [2, 3-d] pyrimidin-6-one and 7-(α- methylbenzyl)-4-chloro [2, 3-d] pyrimidin-6-one were synthesized by the reaction of methyl ...