Academy of Scientific and Innovative Research (AcSIR) , CSIR-HRDC Campus, Joggers Road , Kamla Nehru Nagar , Ghaziabad , Uttar Pradesh 201 002 , India.
J Org Chem. 2019 Dec 6;84(23):15389-15398. doi: 10.1021/acs.joc.9b02141. Epub 2019 Nov 21.
Herein, we report commercially available carbon-supported-palladium (Pd/C)-catalyzed -methylation of nitroarenes and amines using MeOH as both a C1 and a H source. This transformation proceeds with high atom-economy and in an environmentally friendly way via borrowing hydrogen mechanism. A total of >30 structurally diverse -methylamines, including bioactive compounds, were selectively synthesized with isolated yields of up to 95%. Furthermore, selective -methylation and deuteration of nimesulide, a nonsteroidal anti-inflammatory drug, were realized through the late-stage functionalization.
在此,我们报告了一种商业可得的碳负载钯(Pd/C)催化的硝基芳烃和胺的 - 甲基化反应,使用甲醇作为 C1 和 H 源。该转化通过借氢机制以高原子经济性和环保的方式进行。总共合成了超过 30 种结构多样的 - 甲基胺,包括生物活性化合物,其分离收率高达 95%。此外,通过后期功能化实现了非甾体抗炎药尼美舒利的选择性 - 甲基化和氘代。