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报道了氨基磺酸作用下,通过Pictet-Spengler反应合成苯并噻吩并[3′,2′:2,3]吡啶并[4,5-d]噻唑并[3,2-a]嘧啶酮衍生物的有效合成方法.其中,该反应关键中间体7-(3-氨基苯并噻吩-2-基)噻唑并[3,2-a]嘧啶-5-酮,经由7-氯甲基噻唑并[3,2-a]嘧啶-5-酮与2-巯基苯甲腈的烷基化及Thorpe-Ziegler环化制得.该合成过程原料易得,反应条件温和,收率高,为新型稠杂环嘧啶类化合物的合成提供了简便的新途径.
Reported the synthesis of benzothieno [3 ’, 2’: 2,3] pyrido [4,5-d] thiazolo [3,2-a] pyrimidinone by the Pictet-Spengler reaction under the action of aminosulfonic acid (3-aminobenzothiophen-2-yl) thiazolo [3,2-a] pyrimidin-5-one via 7-chloromethylthiazolo [3,2-a] pyrimidin-5-one was alkylated with 2-mercaptobenzonitrile and Thorpe-Ziegler cyclization. The synthesis process was easy to get raw materials, the reaction conditions are mild, high yield, The synthesis of heterocyclic pyrimidines provides a new and convenient way.