- Synthesis, characterization of benzimidazole carboxamide derivatives as potent anaplastic lymphoma kinase inhibitor and antioxidant activity
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Novel benzimidazole carboxamide derivatives have been synthesized and characterized by FTIR, NMR, and mass spectral analysis. The synthesized compounds 7a, 7d, and 7f showed excellent scavenging capacity against DPPH radical and the results are comparable with ascorbic acid. In-silico molecular docking studies exhibited compounds 7a, 7d, and 7f had a good affinity towards the active pocket and the results indicated the ability of potent and selective inhibition of anaplastic lymphoma kinase (ALK) receptor. The theoretical investigation of MEPs, HOMO, LUMO, and the energy gap of HOMO-LUMO were calculated by B3LYP/6-31G method and reactivity descriptors were also computed.
- Sam Daniel Prabu,Lakshmanan, Sivalingam,Ramalakshmi,Thirumurugan,Govindaraj, Dharman,Antony, S. Arul
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p. 266 - 278
(2019/01/19)
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- Candesartan cilexetil preparation method
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The invention provides a novel candesartan cilexetil synthesizing path which comprises the steps of carrying out alkylation reaction on 2-ethoxy benzimidazole-7-alkyl formate and 4-bromomethyl-2'-cyano biphenyl, then hydrolyzing an ester group, then reacting with 1-halogenated ethyl cyclohexyl carbonate ester to obtain an intermediate of 1-[(2'-cyano biphenyl-4-yl) methyl)-2-ethoxy-1H-benzimidazole-7-alkyl carboxylate and then obtaining candesartan cilexetil through tetrazole reaction. The novel candesartan cilexetil synthesizing path disclosed by the invention can finish alkylation, hydrolysis and ester production reaction through a one-pot method and has a few synthesizing steps and simple technology; used raw materials are easy to obtain, production cost is low, three wastes are less, and greenness and environmental friendliness are realized.
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- CRYSTALLINE 1-(CYCLOHEXYLOXYCARBONYLOXY) ETHYL 1-((2'-CYANOBIPHENYL-4-YL)METHYL)-2-ETHOXY-1H-BENZO[D]IMIDAZOLE-7-CARBOXYLATE AND A PROCESS FOR ITS PREPARATION
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The present invention relates to 1-(cyclohexyloxycarbonyloxy)ethyl 1-((2'-cyanobiphenyl-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate in crystalline form and a process for its preparation, which is useful intermediate in the preparation of candesartan cilexetil. The present invention also relates to the preparation of candesartan cilexetil and pharmaceutical composition comprising candesartan cilexetil.
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Page/Page column 25-26
(2008/12/08)
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