Source: http://sioc-journal.cn/Jwk_yjhx/CN/abstract/abstract346543.shtml
Timestamp: 2019-04-24 16:21:14+00:00

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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)-4H-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)-4H-pyrido[1,2-a]pyrimidin-4-one with 2-mercapto-benzonitrile. The structures of the products were characterized by FT-IR, 1H NMR, 13C 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, 5i exhibited more than 93% inhibition rate to Alternaria alternata at 50 mg/L.
徐姣, 马玲, 刘秀波, 马伟, 马岩, 王道林. 新型苯并噻吩稠合吡啶并[1,2-a]嘧啶衍生物的合成及其抑菌活性[J]. 有机化学, 2018, 38(7): 1680-1686.	Xu Jiao, Ma Ling, Liu Xiubo, Ma Wei, Ma Yan, Wang Daolin. Synthesis and Fungicidal Activity of Novel Benzothiophene-Fused Pyrido[1,2-a]pyrimidine Derivatives. Chin. J. Org. Chem., 2018, 38(7): 1680-1686.
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