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Synthesis Of Novel Non-peptide AngⅡ Receptor Antagonists And Studied On Synthesis Of Nitriles And Mercaptocrown

Posted on:2007-02-14Degree:MasterType:Thesis
Country:ChinaCandidate:Y SunFull Text:PDF
GTID:2121360185494169Subject:Organic Chemistry
Abstract/Summary:PDF Full Text Request
Blockade of the rennin-angiotensin system (RAS) is now recognized as an effective approach for the treatment of hypertension and congestive heart failure (CHF). Today, it is possible to antagonise the effects of angiotensin II more specifically by blocking its receptors using non-peptide receptor antagonists. So angiotensin II motivate people to further studies. The design and synthesis, of4`[(1,4-dimethyl-2`-propyl[2,6`-bi-1-H-benzimidole]-1`-yl)]methyl]1,1`-biphenyl] -2-(4`-chloro -imidazole) is described. The compound was efficiently prepared from the key intermediates, the 4`-(1,4-dimethyl-2`-propyl-2,6`-bi-1-H- benzimidole. The synthesized compound was evaluated by QSAR activities. At last of part 1 we also attempted to explain the possible bioactivities of target compound.We synthesized imidazole substitude terazole compound which used the starting material 4`-methyl-2-cynaobiphenyl. The starting material first hydrolysis to carboxylic acid. Imidazoles from N-acylated r-aminonitriles has been developed. N-Acylated r-aminonitriles were reacted with triphenylphosphine and carbon tetrahalide to afford 2,4-disubstituted 5-halo-1Himidazoles in good yield. Finally, we characterized them by MS, 1HNMR and 13CNMR.
Keywords/Search Tags:non-peptide antagonists, substituted imidazole, microwave, aryl nitriles, mercaptobenzocrown
PDF Full Text Request
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