A simple method for the C-4 alkylation of isoquinolines is described using benzoic acid as a nucleophilic reagent and vinyl ketones as an electrophile. The reaction shows tolerance for substitution at C-3, and C-5-C-8 positions as well as allowing some variation of the vinyl ketone electrophiles. The products contain a carbonyl that can act as a synthetic handle for further manipulations giving esters, amines, or simple alkyl products.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9903316 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.2c04149 | DOI Listing |
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