- Synthesis method of 2-(4-aminophenyl)-5-aminobenzimidazole
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The present invention provides a synthesis method of 2- (4-aminophenyl)-5-aminobenzimidazole, comprising the following steps: step 1, preparation of N,N'-bis (4-nitro - α- chlorinated) phenylmethylene p-phenylenediamine; step 2, using N, N'-bis(4-nitro - α- chloro) phenylmethylene p-phenylenediamine preparation N, N'-bis (4-nitro - α - imino) benzyl p-phenylenediamine; step 3, using N, N'-di (4-nitro - α - imino) benzyl p-phenylenediamine preparation 2- ( Step 4, 2-(4-nitro)phenyl-5-aminobenzimidazole was hydrogenated with a hydrogenation catalyst and hydrogen to give 2-(4-amino)phenyl-4-aminobenzimidazole. The present invention is intended to achieve a low production cost and high safety, less harmful pollutants 2- (4-aminophenyl) -5-aminobenzimidazole synthesis method.
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- HCV NS5A replication complex inhibitors. Part 3
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In a recent disclosure,1 we described the discovery of dimeric, prolinamide-based NS5A replication complex inhibitors exhibiting excellent potency towards an HCV genotype 1b replicon. That disclosure dealt with the SAR exploration of the peripheral region of our lead chemotype, and herein is described the SAR uncovered from a complementary effort that focused on the central core region. From this effort, the contribution of the core region to the overall topology of the pharmacophore, primarily vector orientation and planarity, was determined, with a set of analogs exhibiting 50 in a genotype 1b replicon assay.
- Lopez, Omar D.,Nguyen, Van N.,St. Laurent, Denis R.,Belema, Makonen,Serrano-Wu, Michael H.,Goodrich, Jason T.,Yang, Fukang,Qiu, Yuping,Ripka, Amy S.,Nower, Peter T.,Valera, Lourdes,Liu, Mengping,O'Boyle II, Donald R.,Sun, Jin-Hua,Fridell, Robert A.,Lemm, Julie A.,Gao, Min,Good, Andrew C.,Meanwell, Nicholas A.,Snyder, Lawrence B.
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p. 779 - 784
(2013/02/25)
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- SYNTHESIS OF SYMMETRICAL TEREPHTHALOYL DERIVATIVES OF 2-(p-AMINOPHENYL)-5-AMINOBENZIMIDAZOLES - MONOMERS FOR THE PREPARATION OF POLYAMIDES
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Various methods for the synthesis of symetrical terephthaloyl derivatives of 2-(p-aminophenyl)-5-aminobenzimidazoles were studied.Acylation of the isomeric aminonitro-2-phenylbenzimidazoles obtained in this research with subsequent reduction of the nitro groups was found to be the most preparatively convenient method.
- Gel'mont, M. M.,Akulin, Yu. I.,Strelets, B. Kh.,Efros, L. S.
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p. 786 - 792
(2007/10/02)
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