Zhang Xin, Wang Fucheng, Tan Choon-Hong
West China School of Public Health and West China Fourth Hospital, and State Key Laboratory of Biotherapy, Sichuan University, 610041 Chengdu, China.
School of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, 21 Nanyang Link, 637371 Singapore.
JACS Au. 2023 Feb 28;3(3):700-714. doi: 10.1021/jacsau.2c00626. eCollection 2023 Mar 27.
Sulfur can form diverse S(IV) and S(VI) stereogenic centers, of which some have gained significant attention recently due to their increasing use as pharmacophores in drug discovery programs. The preparation of these sulfur stereogenic centers in their enantiopure form has been challenging, and progress made will be discussed in this Perspective. This Perspective summarizes different strategies, with selected works, for asymmetric synthesis of these moieties, including diastereoselective transformations using chiral auxiliaries, enantiospecific transformations of enantiopure sulfur compounds, and catalytic enantioselective synthesis. We will discuss the advantages and limitations of these strategies and will provide our views on how this field will develop.
硫能够形成多种S(IV)和S(VI)手性中心，其中一些由于在药物研发项目中作为药效基团的应用日益广泛，最近受到了极大关注。以对映体纯形式制备这些硫手性中心颇具挑战性，本综述将讨论已取得的进展。本综述总结了用于这些部分不对称合成的不同策略及部分实例，包括使用手性助剂的非对映选择性转化、对映体纯硫化合物的对映体特异性转化以及催化对映选择性合成。我们将讨论这些策略的优缺点，并对该领域的发展方向发表看法。
