01888nas a2200169   4500008004100000022001400041245010100055210006900156260011000225300001200335490000600347520116300353100002501516700002501541700002601566856012601592       2007                        eng d  a1463-926200aNovel one-pot three-component synthesis of 2,4-disubstituted-3H-benzo[b][1,4]diazepines in water0 aNovel onepot threecomponent synthesis of 24disubstituted3Hbenzob  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcNOV  a146-1520 v93 a<p>A novel green and efficient one-pot three-component synthesis of 2,4-disubstituted-3H-benzo[b][1,4]diazepines in excellent isolated yields has been reported. The methodology initially involves the formation of ynones via coupling of a wide range of acid chlorides with terminal alkynes catalysed by Pd(OAc)(2) under copper-, ligand- and solvent-free conditions in just 10 min at rt followed by the Michael addition and cyclocondensation of o-phenylenediamines added in situ using water as a solvent at reflux temprature. In addition, the structure of the benzodiazepine was confirmed to be the diimino molecule and not the enamine by X-ray crystallographic analysis of the benzodiazepine 4b. The methodology is suitable for the operation in combi-chem mode to generate libraries of a diverse array of benzodiazepines. The methodology has been successful in achieving the twin green chemistry objectives of a solvent and ligand free operation and the use of water as a non-hazardous, inexpensive and readily available solvent in the sequential reaction steps performed in situ, thus combining the features of both economic and environmental advantages.</p>1 aPalimkar, Sanjay, S.1 aLahoti, Rajgopal, J.1 aSrinivasan, Kumar, V.  uhttps://library.ncl.res.in/content/novel-one-pot-three-component-synthesis-24-disubstituted-3h-benzob14diazepines-water-1