K2S2O8-mediated coupling of 6-amino-7-aminomethyl-thiazolino-pyridones with aldehydes to construct amyloid affecting pyrimidine-fused thiazolino-2-pyridones.
K2S2O8-mediated coupling of 6-amino-7-aminomethyl-thiazolino-pyridones with aldehydes to construct amyloid affecting pyrimidine-fused thiazolino-2-pyridones.
复制标题
K2S2O8 介导的 6-氨基-7-氨基甲基-噻唑啉代-2-吡啶酮与醛的偶联，构建影响嘧啶融合的噻唑啉代-2-吡啶酮的淀粉样蛋白。
DOI：
10.1039/d1ob01580j
复制
发表时间：
2021
影响因子：
3.2
通讯作者：
Almqvist,Fredrik
中科院分区：
文献类型：
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作者：
Bharate,JaideepB;Ådén,Jörgen;Gharibyan,Anna;Adolfsson,DanE;Jayaweera,SanduniWasana;Singh,Pardeep;Vielfort,Katarina;Tyagi,Mohit;Bonde,Mari;Bergström,Sven;Olofsson,Anders;Almqvist,Fredrik
本文通过K2S2O8介导的6-amino-7-(aminomethyl)-thiazolino-2-pyridones与醛的氧化偶联反应合成了不同功能化的嘧啶并噻唑并2-吡啶酮。所开发的方法温和，底物范围广，不需要过渡金属催化剂或碱。一些合成的化合物能够抑制与阿尔茨海默病相关的淀粉样蛋白-β纤维的形成，而其他化合物则与成熟的淀粉样蛋白-β和α-突触核蛋白纤维结合。
We herein present the synthesis of diversely functionalized pyrimidine fused thiazolino-2-pyridones via K2S2O8-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.