A facile access to 1-substituted and unsubstituted 3-isoquinolinones via Mannich or Sn2 initiated cascade reactions under catalyst-free conditions

在无催化剂条件下,通过曼尼希反应或Sn2引发的级联反应,可简便地合成1-取代和未取代的3-异喹啉酮。

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Abstract

Herein we report new cascade processes for the easy access to 1-substituted and C-unsubstituted 3-isoquinolinones. The Mannich initiated cascade reaction led to the synthesis of novel 1-substituted 3-isoquinolinones under catalyst-free conditions in the presence of nitromethane and dimethylmalonate as nucleophiles without the use of any solvent. The optimization of the synthesis of the starting material in a more environmentally benign manner, allowed the identification of a common intermediate useful for the synthesis of C-unsubstituted 3-isoquinolinones as well. The synthetic utility of 1-substituted 3-isoquinolinones was also demonstrated.

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