Center of Excellence for Innovation in Chemistry (PERCH-CIC), Department of Chemistry, Faculty of Science, Mahidol University, Bangkok 10400, Thailand.
Org Biomol Chem. 2018 Jan 17;16(3):424-432. doi: 10.1039/c7ob02860a.
A highly efficient protocol for a direct thiolation of N-substituted pyrazolones with diaryl disulfides is described. Using a combination of DABCO and silver(i) acetate, the C-S bond formation proceeds smoothly at room temperature under mild and easy to handle conditions. This synthetic strategy offers a convenient and direct modification of antipyrine and other pyrazolone substrates, giving a series of aryl sulfide-substituted pyrazolone products in moderate to excellent yields.
本文描述了一种高效的将 N-取代吡唑酮与二芳基二硫醚进行直接巯基化的方法。该方法使用 DABCO 和醋酸银(i)的组合，在室温下、温和且易于操作的条件下，C-S 键的形成能够顺利进行。该合成策略为安替比林和其他吡唑酮底物提供了一种方便直接的修饰方法，以中等至优异的收率得到一系列芳基硫代吡唑酮产物。
