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A series of N , O -disubstituted glycolamide derivatives have been successfully synthesized through Vilsmeier reagent initialed sequential one-pot multicomponent procedure from α-chloro N -arylacetamides with formamide/PBr 3 and acid chloride. The three-step synthesis involved Vilsmeier formyloxylation reaction, decarbonylation, and esterification. The strategy was also applicable to α-chloro N -(naphthalenyl)acetamide to prepare the corresponding N , O -disubstituted glycolamide products. All of N , O -disubstituted glycolamides were evaluated against dipeptidyl peptidase 4 inhibitory activity. Based on the inhibitory results, several of O -furan-2-carbonyl and O -quinoline-8-sulfonyl N -aryl glycolamide compounds possessed the better effective inhibition of dipeptidyl peptidase 4. |
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