Abstract
Methodology has been developed for the synthesis of C4‐carba‐bridged cystine analogues with a 1,3‐disubstituted phenyl group inserted into the chain. Stereoselective bromobenzylation of the Schöllkopf chiron and a subsequent bromine‐lithium exchange provided a lithiated species for conversion to a higher order cyanocuprate. The latter was cross‐coupled with an α‐bromoacylaminoacetate. Subsequent mild acid hydrolysis provided orthogonally protected amino acids.
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