香草酸甲酯置于氯化亚砜,氨,水,溴,Sodium Ethanolate,Potassium Carbonate,溶剂黄146,Sodium Hydroxide,三氯氧磷体系中,用 甲醇,乙醇,乙酸酐,二甲基亚砜,N,N-二甲基甲酰胺 用作溶剂,化学反应 31.0H,反应生成4-氯-7-(3-氯丙氧基)-3-氰基-6-甲氧基喹啉
参考文献:A New And Practical Synthesis Of Bosutinib
标题:A New And Practical Synthesis Of Bosutinib
摘要:New And Improved Synthetic Route Of Bosutinib Is Described On A Decagram Scale. An Intramolecular Cyclization Of 3-Amino-2-(2-Bromobenzoyl)-Acrylonitrile (22) In K2Co3/dmf Condition To Form The Key 3-Cyano-4-Hydroxyquinoline Intermediate (13) Is Adopted As The Key Step. Bosutinib Is Obtained In 13.7% Yield Over Ten Steps And 98.9% Purity (HPLC),Which Make It As A Process Of Cost Effective,Environmentally Friendly And Feasible For Scale-Up Operation.
Doi:10.3987/com-14-13117