Jiao Xu, Ling Ma, L. Xiubo
Apr 12, 2018
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Journal
Chinese Journal of Organic Chemistry
Abstract
A series of novel benzothieno[3',2':2,3]pyrido[4,5- d ]pyrido[1,2- a ]pyrimidines are prepared via Pictet-Spengler reaction of 2-(3-aminobenzothiophene-2-yl)-4 H -pyrido[1,2- a ]pyrimidin-4-one using sulfamic acid as a catalyst, which in turn were obtained from the Thorpe-Ziegler isomerization of 2-(chloromethyl)-4 H -pyrido[1,2- a ]pyrimidin-4-one with 2-mercapto-benzonitrile. The structures of the products were characterized by FT-IR, 1 H NMR, 13 C NMR spectra and elemental analysis. The fungicidal activities of the prepared compounds were also preliminarily evaluated. For example, 5b exhibited more than 96% inhibition rate to Botrytis cinerea and Gibberella zeae at 50 mg /L, 5f exhibited 98% inhibition rate to Sclerotonia sclerotiorum at 50 mg/L, and 5g , 5 i exhibited more than 93% inhibition rate to Alternaria alternata at 50 mg/L.