Department of Chemistry, Umeå University, 901 87 Umeå, Sweden.
Department of Medical Biochemistry and Biophysics, Umeå University, 901 87 Umeå, Sweden.
Org Biomol Chem. 2021 Nov 18;19(44):9758-9772. doi: 10.1039/d1ob01580j.
We herein present the synthesis of diversely functionalized pyrimidine fused thiazolino-2-pyridones KSO-mediated oxidative coupling of 6-amino-7-(aminomethyl)-thiazolino-2-pyridones with aldehydes. The developed protocol is mild, has wide substrate scope, and does not require transition metal catalyst or base. Some of the synthesized compounds have an ability to inhibit the formation of Amyloid-β fibrils associated with Alzheimer's disease, while others bind to mature amyloid-β and α-synuclein fibrils.
我们在此展示了不同官能化的嘧啶并噻唑啉-2-吡啶酮的合成，这是通过 KSO 介导的 6-氨基-7-(氨甲基)-噻唑啉-2-吡啶酮与醛的氧化偶联反应得到的。所开发的方法温和，具有广泛的底物范围，并且不需要过渡金属催化剂或碱。一些合成的化合物具有抑制与阿尔茨海默病相关的淀粉样β纤维形成的能力，而其他化合物则与成熟的淀粉样β和α-突触核蛋白纤维结合。
