Kong, Jiahui published the artcilePreparation of the key dolutegravir intermediate via MgBr2-promoted cyclization, Synthetic Route of 22483-09-6, the main research area is dolutegravir intermediate preparation; MgBr2-promoted cyclization; chemoselectivity; dolutegravir.
A novel approach for synthesizing the key dolutegravir intermediate is described via MgBr2-promoted intramol. cyclization. Condensation of com. available Me oxalyl chloride and Et 3-(N,N-dimethylamino)acrylate afforded the vinylogous amide in an excellent yield. Subsequent substitution by aminoacetaldehyde di-Me acetal and Me bromoacetate gave rise to the expected precursor for cyclization, which was promoted by MgBr2 to highly selectively convert into pyridinone diester. The key dolutegravir intermediate was finally prepared by the selective hydrolysis of the corresponding diester via LiOH.
Molecules published new progress about Heterocyclization. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Synthetic Route of 22483-09-6.
Referemce:
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