A straightforward methodology for the enantioselective synthesis of 1,2-dihydrophthalazines dearomatization of phthalazines by anion-binding catalysis has been developed. The process involves the Mannich-type addition of silyl ketene acetals to generated -acylphthalazinium chlorides using a -leucine derived thiourea as a H-bond donor catalyst. Ensuing selective and high-yielding transformations provide appealing dihydro- and tetrahydro-phthalazines, phthalazones, and piperazic acid homologues, en route to biologically relevant molecules.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10729020 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.3c03325 | DOI Listing |
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