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. 2012 Jan 1;22(1):278–284. doi: 10.1016/j.bmcl.2011.11.017

Scheme 1.

Scheme 1

The intermediates 8a and 8b were prepared by coupling the carboxylic acid 6 and the diamines 7 (PyBOP, iPr2NEt, DMF); partial (ca. 20%) epimerization was observed and all bivalent derivatives were consequently isolated as mixtures of diastereoisomers.