Abstract
A highly efficient synthesis of the selective endothelin‐converting enzyme, CGS 35066 is described. The key steps involved a Pd‐catalyzed coupling of the phenyl rings of a diphenyl ether, and the use of the Schöllkopf reagent, (2R)‐2‐isopropyl‐3,6‐dimethoxy‐2,5‐dihydropyrazine as a chiral auxiliary furnishing a dibenzofuranylmethyl substituted amino ester in high (>98%) enantiomeric purity, which was then carried forward to complete the synthesis of the ECE inhibitor CGS 35066.
Acknowledgment
Mayo Foundation's research support is gratefully acknowledged.