发明名称 |
A PROCESS FOR THE SYNTHESIS OF BISBENZIMIDAZOLES AND THEIR DERIVATIVES. |
摘要 |
<p>A process for the synthesis of bisbenzimidazoles and its derivations comprising; (i) reacting 5 chloroaniline with zinc dust and acetic anhydride to produce 5 chloroacetanilide; (ii) reacting 5 chloroacetanilide with HN03 to produce 2-nitro-5-chloroacetanilide; (ix) adding sodium methoxide to 2-nitro-5-ch1oroaniline; (x) heating 2-nitro-5-chloroaniline, methyl piperazine, anhydrous K2CO3 and Dimethyl formamide at 100-120°C produce a mixture which is cooled by pouring ice and is filtered to obtain 5-(4'-methylpiperazin-1'-yl)-2-nitroaniline; (xi) treating 5-(4'-methylpiperazin-l'yl)-2-nitroaniline with Pd/C to produce 2-amino-4-(4'-methylpiperazin-1'-yl) aniline; (xii) refluxing a mixture of 2-amino-4-(4'-methylpiperazin-1'yl) aniline and ethyl-4-amino-3-nitrobenzenecarboximidate hydrochloride in presence of ethanol/glacial acetic acid to produce 4-[5'-(4"-methylpiperazin-1"-yl) 15 benzimidazol-2'-yl)-2-nitroaniline; (xiii) treating a solution of 4-[5'-(4"-methylpiperazin-1"-yi) benzimidazol-2'-yl)-2-nitroaniline with palladium on carbon to yield 2-amino-4-[5'-(4"-Methylpiperazin-1"-yl)benzimidazol-2'-yl]aniline; (xiv) heating 2-amino-4-[5'-(4"-Methylpiperazin-1"-yl)benzimidazol-2'-yl]aniline and 3-4-dimethoxy benzaldehyde using nitrobenzene as a solvent at 110-150°C to produce (DMA) i.e 5-(4-methylpiperazin-1-yl)-2-[2'-(3,4-dimethoxyphenyl)-5'-benzimidazolyl] benzimidazole; (ix) heating 2-amino-4-[5'-(4"-Methylpiperazin-1"-yl) benzimidazol-2'-YI] aniline and 5-Formyl-[3-methoxy-4-hydroxy benzimidazole] using nitrobenzene at 110°C to 150°C in presence of argon to produce (TBZ) i.e 5-(4-methylpiperazine-1-yl)-2-[2' (2"-(4-hydroxy-3methoxyphenyl)5"benzimidazolyl) -5'- benzimidazolyl] benzimidazole.</p> |
申请公布号 |
EP1590332(B1) |
申请公布日期 |
2011.04.27 |
申请号 |
EP20030815133 |
申请日期 |
2003.09.08 |
申请人 |
UNIVERSITY OF DELHI |
发明人 |
JAIN, AKASH;TAWAR, URMILA;CHANDRA, RAMESH;DWARAKANATH, B.S.;CHAUDHURY, N. K.;TANDON, VIBHA |
分类号 |
C07D235/18;C07D235/20 |
主分类号 |
C07D235/18 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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