Organic Letters
Organic Letters
5 years ago

Formal [3 + 4] Annulation of α,β-Unsaturated Acyl Azoliums: Access to Enantioenriched N–H-Free 1,5-Benzothiazepines

Formal [3 + 4] Annulation of α,β-Unsaturated Acyl Azoliums: Access to Enantioenriched N–H-Free 1,5-Benzothiazepines
Jindong Zhu, Ding Du, Tao Lu, Kewen Sun, Chao Fang
An unprecedented formal [3 + 4] annulation of α,β-unsaturated acyl azoliums with 2-aminobenzenethiols has been utilized to synthesize enantioenriched N–H-free 1,5-benzothiazepines, which are recognized as privileged structures in numerous biologically active scaffolds. This protocol offers a rapid and direct pathway to access the target compounds with high enantioselectivities and has been applied in the concise synthesis of chiral drug (R)-thiazesim.

Publisher URL: http://dx.doi.org/10.1021/acs.orglett.7b01457

DOI: 10.1021/acs.orglett.7b01457

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