Journal
MOLECULES
Volume 26, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/molecules26102850
Keywords
dolutegravir; MgBr2-promoted cyclization; chemoselectivity
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A novel method for synthesizing the key dolutegravir intermediate is described using MgBr2-promoted intramolecular cyclization, resulting in a highly selective conversion process with excellent yield.
A novel approach for synthesizing the key dolutegravir intermediate is described via MgBr2-promoted intramolecular cyclization. Condensation of commercially available methyl oxalyl chloride and ethyl 3-(N,N-dimethylamino)acrylate afforded the vinylogous amide in an excellent yield. Subsequent substitution by aminoacetaldehyde dimethyl acetal and methyl 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.
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