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-101625nas a2200217   4500008004100000022001400041245010200055210006900157260008600226300001400312490000700326520081000333653001701143653001601160653002101176653002301197100002101220700001801241700002601259856012201285       2008                        eng d  a0039-791100aNovel process for the synthesis of class I antiarrhythmic agent (+/-)-cibenzoline and its analogs0 aNovel process for the synthesis of class I antiarrhythmic agent   a325 CHESTNUT ST, SUITE 800, PHILADELPHIA, PA 19106 USAbTAYLOR & FRANCIS INCcAUG  a2967-29820 v383 a<p>Synthesis of (+/-)-cibenzoline and its analogs has been achieved by a simple sequence of reactions. The diaryl cyanoolefin intermediate 3 could be prepared by Knoevenagel condensation of benzophenone with ethylcyanoacetate to form the tetra-substituted olefin intermediate 2 followed by Krapcho deethoxycarbonylation or from beta-hydroxynitrile intermediate 2' followed by the elimination of hydroxyl group respectively. The 2,2-diphenylcyclopropanecarbonitrile 4 was synthesized from intermediate 3 by cyclopropanation, which was converted to (+/-)-2-(2,2-diphenylcyclopropyl)-2-imidazoline 5 by reaction with ethylenediamine in the presence of a catalytic amount of sulfur. Moreover, the obtained 2-imidazolines were smoothly oxidized to the corresponding imidazoles 6 in good to moderate yields.</p>10aBenzophenone10acibenzoline10acyclopropanation10adiaryl cyanoolefin1 aGholap, Atul, R.1 aPaul, Vincent1 aSrinivasan, Kumar, V.  uhttps://library.ncl.res.in/content/novel-process-synthesis-class-i-antiarrhythmic-agent-cibenzoline-and-its-analogs-0