[4+2+1] Domino cyclization in water for chemo- and regioselective synthesis of spiro-substituted benzo[b]furo[3,4-e][1,4]diazepine derivatives
作者:Chuang Cheng、Bo Jiang、Shu-Jiang Tu、Guigen Li
DOI:10.1039/c1gc15183e
日期:——
has been developed for the synthesis of spiro-substituted benzo[b]furo[3,4-e][1,4]diazepine derivatives. The reaction is a multicomponent domino green process and can be readily performed by reacting inexpensive starting materials of benzene-1,2-diamines, tetronic acid and 2,2-dihydroxy-2H-indene-1,3-dione in aqueous solution under microwave irradiation. The present synthesis shows attractive characteristics
新的区域和化学选择性[4 + 2 + 1]多米诺骨牌 环化已经开发了由两个螺环和五个σ键形成的化合物,用于合成螺取代的苯并[ b ]呋喃[3,4- e ] [1,4]二氮杂卓衍生物。该反应是一种多组分的多米诺绿色工艺,可以通过使廉价的苯1,2-二胺起始原料进行反应而轻松进行,十四酸 和 2,2-二羟基-2 H-茚-1,3-二酮在微波辐射下的水溶液中。本合成显示出吸引人的特性,例如使用水作为反应介质,可以方便地进行一锅操作,缩短反应时间10-18分钟,减少废物产生,而无需使用任何强酸或金属促进剂。这种综合功能很好地补充了GAP(Group-Assistant-纯化)化学,其中通过色谱法和重结晶 可以避免,纯净的产品只需将95%的粗产品洗涤即可 乙醇。