Organic Process Research and Development p. 62 - 66 (2018)
Update date:2022-08-29
Topics:
Liu, Xiangyu
Zhu, Guoqing
Li, Lingai
Liu, Yaowei
Wang, Feng
Song, Xiaoping
Mao, Yongjun
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.
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