Department of Discovery Chemistry, Merck & Co., Inc., South San Francisco, California 94080, United States.
Process Research and Development, Merck & Co., Inc., South San Francisco, California 94080, United States.
Org Lett. 2021 Feb 5;23(3):943-947. doi: 10.1021/acs.orglett.0c04141. Epub 2021 Jan 8.
We provide an account of synthetic strategies aimed at the efficient preparation of 4-amino-4-methyltetrahydro-2-thiopyran 1,1-dioxide (), an important cyclic sulfone building block for medicinal chemistry. A practical and scalable protocol has been developed that readily gives access to the title compound from commercially available and inexpensive starting materials. In addition, this novel approach has enabled the synthesis of various related 4,4-disubstituted cyclic sulfone derivatives that serve as valuable structural motifs for drug discovery.
我们提供了一种旨在高效制备 4-氨基-4-甲基四氢-2-硫代吡喃 1,1-二氧化物（）的合成策略的说明，这是一种用于药物化学的重要环状砜构建块。已经开发出一种实用且可扩展的方案，可从商业上可获得且廉价的起始材料轻松获得标题化合物。此外，这种新方法还能够合成各种相关的 4,4-二取代环状砜衍生物，这些衍生物是药物发现的有价值的结构基序。
