Herein, we present a novel C(sp)-C(sp) bond-forming protocol via the reductive coupling of abundant tertiary amides with organozinc reagents prepared from their corresponding alkyl halides. Using a multistep fully automated flow protocol, this reaction could be used for both library synthesis and target molecule synthesis on the gram-scale starting from bench-stable reagents. Additionally, excellent chemoselectivity and functional group tolerance make it ideal for late-stage diversification of druglike molecules.
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| http://dx.doi.org/10.1021/acs.orglett.3c01390 | DOI Listing |
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