Sherwood, Alexander M.; Burkhartzmeyer, Elise K.; Williamson, Samuel E.; Faley, Michael T.

DOI: PMID:

Abstract

A divergent two-step process has provided access to optically pure enantiomers of MDMA and MDA, clin. relevant phenylisopropylamine entactogens. Target compounds were synthesized from com. available alanine-derived aziridines. Critical process parameters were identified, and the reactions were optimized to avoid chromatog. purifications toward gram-scale isolations, providing (R)-(-)-MDMA, (S)-(+)-MDMA, (R)-(-)-MDA, and (S)-(+)-MDA each in greater than 98% purity by UPLC, >99% enantiomeric excess, and net yields between 50 and 60% for the complete process.

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