Highly Enantiospecific Borylation for Chiral α-Amino Tertiary Boronic Esters
Herein we report a highly efficient and enantiospecific borylation method to synthesize a wide range of enantiopure (>99 % ee) α-amino tertiary boronic esters. The configurationally stable α-N-Boc substituted tertiary organolithium species and pinacolborane (HBpin) underwent enantiospecific borylation at ?78 °C with the formation of a new stereogenic C?B bond. This reaction has a broad scope, enabling the synthesis of various α-amino tertiary boronic esters in excellent yields and, importantly, with universally excellent enantiospecificity (>99 % es) and complete retention of configuration.
BENZIMIDAZOLYL-ACETAMIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS
This invention relates to novel benzimidazolyl-acetamide derivatives to formula (l) and their use as modulators of small-conductance calcium-activated potassium channels (SK channels). Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
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(2013/07/25)
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