Enantioselective Propargylic Amination and Related Tandem Sequences to α-Tertiary Ethynylamines and Azacycles
Jian Zhou reports on enantioselective propargylic amination reactions and related tandem sequences.
Optically active amines and azacycles are widely present in drugs, bioactive compounds and agrochemicals. The synthesis of chiral α-tertiary amines and related azacycles in sufficient structural diversity is important for drug development but constitutes a long-term challenge confronting organic chemists. Professor Jian Zhou from East China Normal University (P. R. of China) said that “enantioenriched α-tertiary propargylamines featuring an α-ethynyl substituent are valuable platform molecules, because their sp C–H bonds and C–C triple bonds permit versatile diversifying reactions.” HE added: “Nevertheless, their facile access is undeveloped in terms of enantioselectivity, substrate scope and synthetic efficiency, as compared with internal proparygylamines.”
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