Synthesis of 1(2H)-Isoquinolones by the Nickel-Catalyzed Denitrogenative Alkyne Insertion of 1,2,3-Benzotriazin-4(3H)-ones.

[摘要]：1,2,3-Benzotriazin-4(3H)-ones reacted with internal and terminal alkynes in the presence of a nickel(0)/phosphine catalyst to give a wide range of substituted 1(2H)-isoquinolones, e.g., I (R1 = Me, Bn, Ph, 4-Me-Ph, 4-MeO-Ph, 4-CF3-Ph; R2 = Ph, CH2OBn, 4-CF3-Ph, 4-MeO-Ph, CO2Et, Bpin; R3 = Me, i-Pr, n-Pr, n-Bu, TMS, Ph, CH2OBn; Ph,), in high yield. The reaction proceeded through denitrogenative activation of the triazinone moiety and the following insertion of alkynes.

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