含有不同取代基的(E)-2-(苯并噻唑-2-基)-3-(2-羟基苯基)丙烯腈与亚磷酸二苯酯在水中,无催化剂催化即可发生Michael加环/环化串联反应,可以高产率地生成相应的[2-氨基-3-(苯并噻唑-2-基)-4胁色烯-4-基]膦酸酯衍生物.同时,也尝试了水杨醛、2-(苯并噻唑-2-基)乙腈和亚磷酸二苯酯在Et3N催化下的三组分一锅法反应合成相应的膦酸酯衍生物.
A series of (2-amino-3-(benzothiazol-2-yl)-4H-chromen-4-yl)phosphonate derivatives were synthesized in good to excellent yields by Michael addition/cyclization of diphenyl phosphite to diverse substituted (E)-2-(benzothiazol-2-yl)-3-(2- hydroxyphenyl)acrylonitriles under catalyst-free condition in water. Meanwhile, one-pot three component reaction of salic- ylaldehyde, 2-(benzothiazol-2-yl)acetonitrile and diphenyl phosphate was also tested using Et3N as catalyst to synthesize these phosphonate derivatives