Institute of Pharmaceutical Science and Technology, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China.
Zhejiang Hisoar Pharmaceutical Co., Ltd, Taizhou 318000, China.
Chem Commun (Camb). 2022 Jun 9;58(47):6765-6768. doi: 10.1039/d2cc01731h.
A new type of organocatalyzed 1,3-thiosulfonylation has been developed to straightforwardly access highly functionalized vinyl sulfones, which features mild conditions, atom- and step-economy, practicability, conciseness, and environmental friendliness. Moreover, these valuable products can be transformed to vinyl sulfides a base-promoted isomerization. The versatile route can efficiently and rapidly introduce SCD groups with excellent levels of deuterium content (>99% D) by utilizing our newly developed SCD reagents. Gram-scale operations and further transformations are smoothly carried out, providing promising applications for drug discovery.
一种新型的有机催化 1,3-硫代磺酰化反应已经被开发出来，可以直接构建高官能化的乙烯基砜化合物。该反应具有条件温和、原子经济性和步骤经济性、实用性、简洁性和环境友好性等优点。此外，这些有价值的产物可以通过基促进的异构化转化为乙烯基硫醚。通过利用我们新开发的 SCD 试剂，这种多功能的路线可以高效、快速地引入 SCD 基团，并且氘含量极高（>99% D）。克级规模的操作和进一步的转化也可以顺利进行，为药物发现提供了有前景的应用。
