Environmentally respectful methods for generating and utilizing difluorocarbene (:CF₂) in the synthesis of a wide array of valuable difluoromethylated compounds are disclosed. In particular, the insertion of the CF₂ moiety into aromatic/heteroaromatic alcohols, thiols, olefins, and alkynes under neat or aqueous micellar catalysis conditions is demonstrated. These methods yield both satisfactory results and significantly lower E-Factors compared to traditional synthetic approaches. Key applications of these methodologies include optimization en route to a pantoprazole intermediate and development of a representative one-pot chemoenzymatic sequence. Additionally, analysis via calorimetry indicates no significant safety risk in the context of the developed solvent-free conditions.

中文翻译：

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原位生成的二氟卡宾 （：CF2） 与芳香族/杂芳烃醇、硫醇、烯烃和炔烃在环保条件下的反应


公开了在合成各种有价值的二氟甲基化化合物中生成和利用二氟卡宾 （：CF₂） 的环保方法。特别是，在纯或水性胶束催化条件下，证明了 CF₂ 部分插入芳香族/杂芳香族醇、硫醇、烯烃和炔烃中。与传统的合成方法相比，这些方法既产生了令人满意的结果，又显著降低了 E 因子。这些方法的主要应用包括优化泮托拉唑中间体的途径和开发代表性的一锅法化学酶序列。此外，通过量热法进行的分析表明，在开发的无溶剂条件下没有重大的安全风险。