《An efficient synthesis of 1,5-benzodiazepine derivatives catalyzed by boric acid》.pdfVIP

Available online at Chinese Chemical Letters 20 (2009) 905–908 /locate/cclet An efficient synthesis of 1,5-benzodiazepine derivatives catalyzed by boric acid Xin Zhou, Mei Yue Zhang, Shu Tao Gao, Jing Jun Ma, Chun Wang *, Chao Liu Hebei Key Laboratory of Bioinorganic Chemistry, College of Sciences, Agricultural University of Hebei, Baoding 071001, China Received 20 November 2008 Abstract 1,5-Benzodiazepine derivatives have been synthesized by the condensation of o-phenylenediamines and ketones in the presence of boric acid as catalyst under mild conditions. This method is simple, environmentally benign and high yielding. # 2009 Chun Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. Keywords: 1,5-Benzodiazepines; o-Phenylenediamines; Boric acid; Synthesis Benzodiazepines and their derivatives have attracted considerable attention from researchers, because of their bioactive and pharmaceutical properties. Many members of this family are widely used as anticonvulsant, antianxiety, analgesic, seditative, antidepressive and hypnotic, and anti-inflammatory agents [1]. In addition, 1,5-benzodiazepines have found applications as available intermediates in the synthesis of fused ring compounds such as triazolo-, oxazino- or furano-benzodiazepine [2]. Benzodiazepine derivatives also find commercial use as dyes for acrylic fibers [3]. Therefore, the preparation of benzodiazepines and their derivatives is of much current importance. More recently, lot of methods for the synthesis of 1,5-benzodiazepines are reported in the literature. Generally, they are synthesized by condensa