Development of Safe One-Pot Synthesis of N-1- and C-2-Substituted Benzimidazole via Reductive Cyclization of o-Nitroarylamine Using Na2S2O4

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• 作者：Shinichi Oda ; Hideki Shimizu ; Yasunori Aoyama ; Tatsuo Ueki ; Sumio Shimizu ; Hiroshi Osato ; Yoshiyuki Takeuchi
• 刊名：Organic Process Research & Development
• 出版年：2012
• 出版时间：January 20, 2012
• 年：2012
• 卷：16
• 期：1
• 页码：96-101
• 全文大小：918K
• 年卷期：v.16,no.1(January 20, 2012)
• ISSN：1520-586X

文摘

We report that the reductive cyclization of o-nitroarylamine with aldehyde using sodium dithionite (Na₂S₂O₄) could be accelerated by addition of H₂O, which made it possible to control the heat release of the reaction by semibatch-type operation. Safety evaluation was performed using DSC, ARSST, in situ IR analysis, and Multimax.