Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
J Org Chem. 2010 Jan 1;75(1):265-8. doi: 10.1021/jo902327n.
A simple and practical synthetic method of pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic heterocycles has been developed. Treatment of 2-(2-haloaryl)tetrahydropyrimidines with NaH and a heterocumulene such as carbon disulfide, isothiocyanates, and isocyanates in DMF provides the desired cyclization products through a regioselective S(N)Ar-type reaction. This method provides direct access to PD 404182 and related compounds.
一种简单实用的嘧啶并[1,2-c][1,3]苯并噻嗪-6-亚胺和相关三环杂环的合成方法已经开发出来。用 NaH 和二甲基甲酰胺中的杂cumulene（如二硫化碳、异硫氰酸酯和异氰酸酯）处理 2-(2-卤代芳基)四氢嘧啶，可以通过区域选择性 S(N)Ar 型反应得到所需的环化产物。该方法可直接得到 PD 404182 及相关化合物。
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