Synthesis And Chemical Stability Of Indolizine Derivatives Of Antihypertensive And Antidiabetic Agents.

Research Journal of Pharmaceutical, Biological and Chemical Sciences

article

Basavaraj M¹  Giles D²  Das Ak²  Ganesh S Andhale.² 

[1] Department of Pharmaceutical Chemistry, Vivekananda College of Pharmacy;Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy

关键词: cycloaddition;    chemical stability;    indolizine;    hydrolysis;   

DOI  :  10.33887/rjpbcs/2019.10.4.23

学科分类：工程和技术（综合）

来源: Research Journal of Pharmaceutical, Biological and Chemical Sciences

【 摘 要 】

We have synthesized1,3 substituted indolizines by reacting pyridine, phenacyl bromide andethylpropiolate in presence of triethylamine, in which the key step is the formation of N-acyl pyridinium saltwhich could participate in a [3+2] intramolecular cycloaddition reaction with ethylpropiolate to form anunstable intermediate which instantly facilitates aromatization to form substitutedindolizine. The formedindolizine reacted with hydralazine and metformin to form the derivatives (2a-f). And also we synthesized 1-substituted indolizine, this substituted indolizine formylated to get formylated indolizineand reacted withhydralazine and metformin to form the derivatives (1a-b). All the synthesized derivatives were characterized1 by IR, H NMR and Mass spectral data. The synthesized derivatives were studied for chemical hydrolysis at pH1.2, 6.8, 7.4, and all the derivatives were found be stable at 1.2 pH and partially hydrolyzed at 6.8 andmaximum hydrolysis occurred at 7.4 pH. Among the synthesized prodrugs 2b, 2f were found to be best amongthe series.

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