A new, practical, and convergent synthetic route of gedatolisib, an antitumor agent, is developed on a hectogram scale which avoids the Pd coupling method. The key step is adopting 6-(4-nitrophenyl)-1,3,5-triazine-2,4-diamine and 2,2′-dichlorodiethyl ether to prepare the key 4,4′-(6-(4-nitrophenyl)-1,3,5-triazine-2,4-diyl)dimorpholine in 77% yield and 98.8% purity. Gedatolisib is obtained in 48.6% yield over five simple steps and 99.3% purity (HPLC). Purification methods of the intermediates and the final product involved in the route are given.

中文翻译：

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格达列西的新的实用合成

以百克级规模开发了一种新的，实用且聚合的抗肿瘤药gedatolisib合成路线，该路线避免了Pd偶联方法。关键步骤是采用6-（4-硝基苯基）-1,3,5-三嗪-2,4-二胺和2,2'-二氯二乙醚制备关键的4,4'-（6-（4-硝基苯基） ）-1,3,5-三嗪-2,4-二基）二吗啉的产率为77％，纯度为98.8％。在五个简单的步骤中以98.6％的纯度（HPLC）获得了Gedatolisib的收率为48.6％。给出了该路线涉及的中间体和最终产物的纯化方法。