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

被引:28
|
作者
Oda, Shinichi [1 ]
Shimizu, Hideki [1 ]
Aoyama, Yasunori [1 ]
Ueki, Tatsuo [1 ]
Shimizu, Sumio [1 ]
Osato, Hiroshi [1 ]
Takeuchi, Yoshiyuki [1 ]
机构
[1] Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
关键词
NITRO-COMPOUNDS; THERMAL HAZARDS; POLYMERASE; INHIBITORS; NITROANILINES; DERIVATIVES;
D O I
10.1021/op200251c
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
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.
引用
收藏
页码:96 / 101
页数:6
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