 Functionalized 4- and 6-azaindolines have been prepared in good yield and high enantiomeric excess by the chiral cation-directed asymmetric cyclization of aminopyridine-derived imines via phase-transfer catalysis (up to 97 % yield and 96 % ?ee?). The extension of this methodology to diasteroselective cyclizations has also been investigated.

Asymmetric synthesis of azaindolines via cation-directed cyclization

245th National Meeting (2013)

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