硅烷介导的、使用甲醛的便捷C-H和N-H甲基化反应。
Silane-mediated, facile C-H and N-H methylation using formaldehyde.
作者信息
Khan Jabir, Taneja Neha, Yadav Naveen, Hazra Chinmoy Kumar
机构信息
Department of Chemistry, Indian Institute of Technology Delhi, Hauz Khas, New Delhi, 110016, India.
出版信息
Chem Commun (Camb). 2024 Oct 3;60(80):11367-11370. doi: 10.1039/d4cc03976a.
The use of ()-formaldehyde for the methylation/alkylation of C(sp)-H and N-H bonds, utilizing a combination of silane and hexafluoroisopropanol (HFIP) as activators, is reported. Overcoming the complexity of C(sp)-H methylation on aryl and indole substrates, the process utilizes a Friedel-Crafts alkylation, followed by silane as a hydride donor, under a mild acidic medium. The method has been employed for the synthesis of the antifungal drug butenafine and a derivative of the non-steroidal anti-inflammatory drug (NSAID) flurbiprofen.
据报道，使用（）-甲醛对C（sp）-H和N-H键进行甲基化/烷基化反应，采用硅烷和六氟异丙醇（HFIP）的组合作为活化剂。该方法克服了芳基和吲哚底物上C（sp）-H甲基化的复杂性，在温和酸性介质下，通过傅克烷基化反应，然后以硅烷作为氢化物供体来实现。该方法已用于抗真菌药物布替萘芬和非甾体抗炎药（NSAID）氟比洛芬衍生物的合成。
Zotero 插件