2,4-二氯噻吩并[3,2-d]嘧啶主要作为医药中间体或农药中间体，用于相关药物和农药的合成制备。
医药; 农药
合成路线 1（1. 合成：16234-14-3）
产率：100%
合成条件：for 2 h; Heating / reflux
实验步骤：向尿嘧啶（5g，29mmol）在POCl 3（40mL）中的悬浮液中加入二异丙基乙胺（13mL，74mmol）并将反应物加热回流2小时。 然后通过减压蒸馏除去过量的POCb和二异丙基乙胺，将得到的棕色固体溶解在氯仿中并用水分配。 通过加入5M NaOH使水相呈碱性，再用氯仿萃取两次。 将合并的有机级分用水和盐水洗涤，干燥（Na 2 SO 4），过滤并浓缩，得到产物，为浅棕色固体（6.05g，定量收率）。 1 H NMR（CDCl 3,300MHz）：8.16（d，J = 5.4Hz，1H），7.56（d，J = 5.7Hz，1H）; LRMS（ESI）：m / z计算值[M + H] + 204.94,206.94，实测值205.1,207.0。
参考文献：
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合成路线 2（2. 合成：16234-14-3）
产率：61%
合成条件：With trichlorophosphate In N , N -dimethyl-aniline at 125℃; for 22 h;
实验步骤：将噻吩脲（6.0g）和N，N-二甲基苯胺（2.9mL）在磷酰氯（35mL）中的溶液在125℃（油浴）下在氩气下加热22小时。 将溶液冷却至50℃并在剧烈搅拌下倒入冷水（0℃，8.0mL）中。 过滤沉淀物，用水洗涤，并溶解在EtOAc中。 过滤有机溶液，用水洗涤，有机相用MgSO 4干燥，过滤并浓缩，得到黄色沉淀（4.5g，61％收率）。
参考文献：
- [1] Patent: US2004/14755, 2004, A1. Location in patent: Page/Page column 9
合成路线 3（3. 合成：16234-14-3）
产率：100%
合成条件：at 100℃;
实验步骤：2,4-二氯 - 噻吩并[3,2-d]嘧啶的步骤1A的制备将85mg噻吩并[3,2-d]嘧啶-2,4-二醇（0.5mmol）悬浮于1.25mL POCl 3中。 将混合物在100℃加热过夜。 在减压下除去POCl 3。 将混合物溶于二氯甲烷中并用冰淬灭。 通过用二氯甲烷（2.x.）萃取收集产物。 将合并的有机层用MgSO 4干燥并浓缩，得到定量收率的标题化合物，将其不经进一步纯化用于下一步骤。
参考文献：
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