A series of novel indole and pyrimidine scaffolds bearing 1,2,3‐triazoles have been designed and synthesized using click chemistry reaction conditions. Target compounds 9a‐j were synthesized in the multi‐step process. In the first step 5‐substituted‐1‐methyl‐1H ‐indole‐3‐carbaldehyde 2a‐b reacted with ethyl cyanoacetate 3 and guanidine hydrochloride 4 in presence of L‐Proline in ethanol undergoes cyclisation to form 5a‐b . Further, 5a‐b condensed with various benzaldehydes to form Schiff's base 6a‐f , which further proporgylated with propargyl bromide to form 7a‐f . Finally, 7a‐f was subjected to click‐chemistry with various azides in the presence of CuSO₄.5H₂O + sodium ascorbate mixture in Dimethylformamide at room temperature to obtain 2 + 3 cycloaddition products 9a‐j in high yield. All these synthetic methods are mostly green and inexpensive with excellent yields.

中文翻译：

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一种新的1,2,3-三唑取代的嘧啶衍生物的简便合成

使用点击化学反应条件设计并合成了一系列带有1,2,3-三唑的新型吲哚和嘧啶骨架。在多步过程中合成了目标化合物9a-j。在第一步中，在乙醇中存在L-脯氨酸的情况下，在氰基乙酸乙酯3和盐酸胍4中将5-取代1-甲基1 H-吲哚3-甲醛2a-b与氰基乙酸乙酯3和盐酸胍4反应，进行环化形成5a-b。此外，5a-b与各种苯甲醛缩合形成Schiff碱6a-f，再与炔丙基溴进一步丙烷化形成7a-f。最后，7a-f在室温下，在二甲基甲酰胺中的CuSO ₄ .5H ₂ O +抗坏血酸钠混合物存在下，使用各种叠氮化物进行点击化学反应，以高收率获得2 + 3个环加成产物9a-j。所有这些合成方法大部分都是绿色的，并且价格低廉，且产率高。