Enantioselective amination of 4-alkylisoquinoline-1,3(2 H ,4 H )-dione derivatives.

A mild and efficient enantioselective amination of 4-alkylisoquinoline-1,3(2 H ,4 H )-dione derivatives was established, which is compatible with a broad range of substrates and delivers the final products in excellent yields (up to 99%) and ee values (up to 99%) with low catalyst loading (down to 1 mol%). The synthetic potential of this methodology was also demonstrated in the gram scale level.