9-乙基鸟嘌呤的合成

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以丙二酸二乙酯、盐酸胍为起始原料,在碱性条件下缩合得到中间产物2-氨基-4,6-二羟基嘧啶,然后,以三乙胺为缚酸剂,在80℃下与三氯氧磷反应,再用氢氧化钠分解得到2-氨基-6-氯嘧啶-4(3H)-酮,然后经过乙氨基化、亚硝化、环合反应,得到最终反应产物。并通过优化反应条件,获得了最佳工艺参数。该反应路线操作简便、工艺路线可行。产物经过熔点、IR、~1HNMR、~(13)CNMR等表征确证。 Diethyl malonate and guanidine hydrochloride were used as starting materials to obtain the intermediate product 2-amino-4,6-dihydroxypyrimidine by condensation under basic conditions. Then, triethylamine was used as acid-binding reagent at 80 ℃ Under phosphorus oxychloride reaction, and then sodium hydroxide decomposition to give 2-amino-6-chloropyrimidin-4 (3H) - ketone, and then ethylamino, nitrosation, cyclization reaction, the final reaction product. By optimizing the reaction conditions, the best process parameters were obtained. The reaction route is easy to operate and the process route is feasible. The product was confirmed by melting point, IR, ~ 1HNMR, ~ (13) CNMR.
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