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Frontispiece: Direct and Enantioselective Synthesis of N−H‐Free 1,5‐Benzodiazepin‐2‐ones by an N‐Heterocyclic Carbene Catalyzed [3+4] Annulation Reaction
Author(s) -
Fang Chao,
Cao Jing,
Sun Kewen,
Zhu Jindong,
Lu Tao,
Du Ding
Publication year - 2018
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201880964
Subject(s) - annulation , enantioselective synthesis , carbene , chemistry , catalysis , aryl , combinatorial chemistry , stereochemistry , organic chemistry , alkyl
The 1,5‐benzodiazepin‐2‐one heterocyclic motif is a privileged structure frequently found in numerous natural products and synthetic compounds with diverse biological activities. An N‐heterocyclic carbene‐catalyzed formal [3+4] annulation of α,β‐unsaturated acylazoliums with protecting group‐free aryl 1,2‐diamines is reported by T. Lu, D. Du et al. in their Full Paper on page 2103 ff., for a direct and highly enantioselective synthesis of 4‐aryl N−H‐free 1,5‐benzodiazepin‐2‐ones. The protocol is also scalable and the desired products can easily undergo subsequent derivatizations.

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