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Vilsmeier reagent initialed sequential one-pot multicomponent synthesis of N,O-disubstituted glycolamides as dipeptidyl peptidase 4 inhibitors
A series of N,O-disubstituted glycolamide derivatives have been successfully synthesized through Vilsmeier reagent initialed sequential one-pot multicomponent procedure from alpha-chloro N-arylacetamides with formamide/PBr3 and acid chloride. The three-step synthesis involved Vilsmeier formyloxylation reaction, decarbonylation, and esterification. The strategy was also applicable to alpha-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.
Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Quality Control of Isoxazole-5-carbonyl chloride, you can also check out more blogs about62348-13-4
Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem