A Three-Layer Transformation Strategy toward Functionalized Fused Hydantoins and Diketopiperazines

Organic Letters 2026 Open access

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Authors: Maria-Aikaterini Giannakaki, Marios Zingiridis, Konstantinos G. Froudas, Constantinos G. Neochoritis
DOI: 10.1021/acs.orglett.5c05391
Cited by: 2
References: 68

Abstract

We present mAUCy (modified Asinger-Ugi cyclization), a scalable three-layer strategy enabling rapid synthesis of diverse thiazolo hydantoins and diketopiperazines. Beginning from 3-thiazolines via a modified Asinger reaction, followed by an Ugi-Joullié multicomponent reaction and base-induced annulation, the method delivers complex compounds in less than 3 h. Operable on a multigram scale without chromatography, it allows telescoped one-pot processing, a broad substrate scope, and late-stage modifications. Single-crystal analysis confirmed the scaffold structures.

Fields of Study & Subjects

Synthesis of heterocyclic compounds Multicomponent Synthesis of Heterocycles Coordination Chemistry and Organometallics

Publication details

Journal / source
Organic Letters
Publisher
American Chemical Society (ACS)
Volume
28
Issue
6
Pages
2096–2101
Publication date
30 January 2026
Language
EN