使用选择性磺酰胺化试剂制备磺酸盐和磺酰胺。
Preparation of Sulfamates and Sulfamides Using a Selective Sulfamoylation Agent.
机构信息
Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.
School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.
出版信息
Org Lett. 2021 Apr 2;23(7):2595-2599. doi: 10.1021/acs.orglett.1c00504. Epub 2021 Mar 22.
Sulfamates and sulfamides are prevalent in biological molecules, but their universal synthetic methods are limited. We herein report a sulfamoylation agent with high solubility and shelf stability. Various sulfamates and sulfamides can be synthesized directly from alcohols or amines by employing this agent with high selectivity and high yields. This protocol was also successfully used for late-stage sulfamoylation of pharmaceuticals containing a hydroxyl or amino group.
磺胺酸盐和磺胺类药物在生物分子中很常见，但它们的通用合成方法有限。我们在此报告了一种具有高溶解性和货架稳定性的磺胺化试剂。通过使用该试剂，可以高选择性和高产率直接从醇或胺合成各种磺胺酸盐和磺胺类药物。该方案还成功地用于含羟基或氨基的药物的后期磺胺化。
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