Efficient Construction of Tetrahydroquinazolines via HFIP‐Promoted [1, 5]‐Hydride Transfer/6‐Endo‐Trig Cyclization. Issue 45 (1st December 2022)

• Record Type: Journal Article
• Authors: Dong, Fengying; Song, Xiaopei; Yin, Xiangcong; Wang, Liang
• Is Part Of: ChemistrySelect. Volume 7:Issue 45(2022)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2022-12-01
• Subjects: Cascade Reaction -- Fluorinated Alcohol -- Heterocyclic Compounds -- 1, 5-Hydride Transfer -- Tetrahydroquinazolines; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.202203936
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: Described herein is a practical and scalable protocol for the syntheses of pharmaceutically significant tetrahydroquinazolines in good yields via cascade condensation/[1, 5]‐hydride transfer/6‐endo‐trig cyclization, which features mild, salt‐free & additive‐free conditions; broad substrate scope; and chemoselective N, N ‐dialkylation of primary amine with two diverse alkyl groups in one step. Abstract : A practical and scalable protocol was disclosed for the syntheses of tetrahydroquinazolines via cascade condensation/[1, 5]‐hydride transfer/6‐endo‐trig cyclization, which features mild, salt‐free & additive‐free conditions; broad substrate scope; and chemoselective N, N‐dialkylation of primary amine with two diverse alkyl groups in one step.