二氟甲基化反应研究进展

New Progress in Difluoromethylation

由于向有机化合物中引入氟原子或含氟官能团会引起其理化性质、生物活性等性能的显著改变或提升,而且有机氟化合物在医药、农药和新材料等方面发挥着不可或缺的作用,因此开发各类有机氟化反应具有重要的学术和应用价值。其中,向分子中引入二氟甲基是氟化学的热门研究领域。近年来,各类二氟甲基化试剂以高效、安全、经济的优点应用于二氟甲基化反应中。本文将各类二氟甲基化反应根据其使用的不同二氟甲基化试剂分为含氟甲烷类、TMS类、含氟羧酸及羧酸衍生物类、含氟磷酸酯、含氟砜类、二氟甲基金属试剂以及其他类,较为详细地介绍了近五年来报道的烷烃、芳烃、杂原子等的直接、自由基、卡宾等机制的二氟甲基化反应研究。

Organic fluorine compounds played an indispensable role in medicines,pesticides and new materials due to the introduction of fluorine atoms or fluorine groups into organic compounds,which brought about significant changes or enhancements in their physical and chemical properties,biological activities and other properties.Therefore,the development of various types of organic fluorination reactions had important academic and application value.Among them,the introduction of difluoromethyl groups into molecules was a hot research field in fluorine chemistry.In recent years,various difluoromethylation reagents have been used in difluoromethylation reactions with the advantages of high efficiency,safety and economy.In this paper,the difluoromethylation reaction was divided as fluorinated methane,TMS,fluorine-containing carboxylic acid and carboxylic acid derivatives,fluorine-containing phosphates,fluorine-containing sulfones,difluoromethyl metal reagents,and other types.The direct,radical and Valery Karpin difluoromethylation of alkanes,aromatics and heteroatoms reported in the past five years were reviewed in detail.