Research on Chemical Intermediates p. 1041 - 1045 (2011)
Update date:2022-08-30
Topics:
Luo, Hu
Xia, Wei
Qian, Chao
Chen, Xinzhi
He, Chaohong
8-[4-[4-(2-Pyrimidinyl)-1-piperaziny]butyl]-8-azaspiro [4,5] decane-7,9-dione hydrochloride (buspirone hydrochloride) was obtained in one pot with a 51.8% overall yield. The key intermediate, 1-(2-pyrimidinyl) piperazine, was synthesized through chlorination and cyclization condensation reaction with diethanolamine as initial material. This modified protocol has the notable advantages of mild reaction condition, convenient operation, and high overall yield.
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