



在发展具有原创性的新型亲电氟烷硫基化试剂开展了系统研究,发展了两类共3个亲电三氟甲硫基试剂,其中包括结构独特的三氟甲基次磺酸酯试剂以及目前活性最高的商品化亲电三氟甲硫基糖精试剂,这两个试剂分别被国内外同行称为“吕-沈试剂”(Lu-Shen reagent) 与“沈试剂” (Shen Reagent),发展了首例光学活性亲电三氟甲硫基化试剂,发展了可应用于高效合成[1F]标记的三氟甲硫基化芳烃的亲电溴二氟甲硫基化试剂,解决了温和条件下小分子引入三氟甲硫基的难题;发展了首例亲电二氟甲硫基试剂及首例自由基类型二氟甲硫基试剂,为向有机小分子高效引入二氟甲硫基化提供了新方案;发展了首例自由基类型一氟甲硫基试剂。基于该课题组所发展的一系列亲电氟烷硫基化试剂成立了深圳邦奇氟医学材料有限公司。
Electrophilic fluoroalkylthiolating reagents. Fluoroalkylthio groups often have high Hansch’s hydrophobicity parameter and electronwithdrawing property. For example, the trifluoromethylthio group (-SCF3) is one of the most lipophilic substituents (π = 1.44). The high lipophilicity of the fluoroalkylthio groups may improve drug molecules’ pharmacokinetic and physicochemical properties such as lipophilicity and metabolic stability. The Shen group developed a toolbox of shelf-stable yet high reactive electrophilic fluoroalkylthiolating reagents that are able to deliver the fluoroalkylthio groups sitespecifically to the target molecules.
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