K2S2O8-mediated coupling of 6-amino-7-aminomethyl-thiazolino-pyridones with aldehydes to construct amyloid affecting pyrimidine-fused thiazolino-2-pyridones. Issue 44 (3rd November 2021)

• Record Type: Journal Article
• Authors: Bharate, Jaideep B.; Ådén, Jörgen; Gharibyan, Anna; Adolfsson, Dan E.; Jayaweera, Sanduni Wasana; Singh, Pardeep; Vielfort, Katarina; Tyagi, Mohit; Bonde, Mari; Bergström, Sven; Olofsson, Anders; Almqvist, Fredrik
• Is Part Of: Organic & biomolecular chemistry. Volume 19:Issue 44(2021)
• Page Start: 9758
• Page End: 9772
• Publication Date: 2021-11-03
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/d1ob01580j
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : We herein present the synthesis of diversely functionalized pyrimidine fused thiazolino-2-pyridones via K2 S2 O8 -mediated oxidative coupling of 6-amino-7-(aminomethyl)-thiazolino-2-pyridones with aldehydes. Abstract : We herein present the synthesis of diversely functionalized pyrimidine fused thiazolino-2-pyridones via K2 S2 O8 -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.