Department of Chemistry, Washington State University , Pullman, Washington 99164, United States.
Org Lett. 2017 Jul 21;19(14):3819-3822. doi: 10.1021/acs.orglett.7b01693. Epub 2017 Jul 3.
Sulfinic acids are commonly encountered intermediates found in natural product synthesis and medicinal chemistry. However, because of high reactivity, instability, and harsh reaction conditions, they are difficult to synthesize. Herein we have developed an oxidation-free method to produce sulfinic acids and sulfinate salts using 2-sulfinyl benzothiazole (BTS). We have also demonstrated the synthetic usefulness by developing one-pot syntheses of sulfones and sulfonamides.
亚磺酸是天然产物合成和药物化学中常见的中间体。然而,由于其高反应性、不稳定性和苛刻的反应条件,它们很难合成。在此,我们开发了一种无需氧化的方法,使用 2-亚磺酰基苯并噻唑 (BTS) 来制备亚磺酸和亚磺酸盐。我们还通过一锅法合成砜和磺酰胺证明了其合成用途。