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:
Oda, Shinichi
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Oda, Shinichi
[1
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Shimizu, Hideki
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Shimizu, Hideki
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Aoyama, Yasunori
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Aoyama, Yasunori
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Ueki, Tatsuo
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Ueki, Tatsuo
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Shimizu, Sumio
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Shimizu, Sumio
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Osato, Hiroshi
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Osato, Hiroshi
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Takeuchi, Yoshiyuki
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Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, JapanShionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
Takeuchi, Yoshiyuki
[1
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[1] Shionogi & Co Ltd, Chem Dev Ctr, CMC Dev Labs, Amagasaki, Hyogo 6600813, Japan
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.
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Rutgers State Univ, Ernest Mario Sch Pharm, Dept Med Chem, 160 Frelinghuysen Rd, Piscataway, NJ 08854 USA
Mansoura Univ, Fac Pharm, Dept Med Chem, Mansoura 35516, EgyptRutgers State Univ, Ernest Mario Sch Pharm, Dept Med Chem, 160 Frelinghuysen Rd, Piscataway, NJ 08854 USA
Ali, Ahmed R.
Hu, Longqin
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Rutgers State Univ, Ernest Mario Sch Pharm, Dept Med Chem, 160 Frelinghuysen Rd, Piscataway, NJ 08854 USA
Rutgers Canc Inst New Jersey, New Brunswick, NJ 08901 USARutgers State Univ, Ernest Mario Sch Pharm, Dept Med Chem, 160 Frelinghuysen Rd, Piscataway, NJ 08854 USA
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Curia India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, IndiaCuria India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, India
Cherukumalli, Purna Koteswara Rao
Prasad, Kotipalli Yesu
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Curia India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, IndiaCuria India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, India
Prasad, Kotipalli Yesu
Khanna, Baman
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Curia India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, IndiaCuria India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, India
Khanna, Baman
Srinivas, Ravula
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Curia India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, IndiaCuria India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, India
Srinivas, Ravula
Vijayasaradhi, Sivalenka
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Curia India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, IndiaCuria India Pvt Ltd, Albany Mol Res Hyderabad Res Ctr, Plot 9,MN Pk, Hyderabad 500078, India