A Cu-promoted reaction of β-keto trifluoromethyl amines enabling stereoselective synthesis of trifluoromethylated aziridines-Reference-Cited by-同舟云学术

A Cu-promoted reaction of β-keto trifluoromethyl amines enabling stereoselective synthesis of trifluoromethylated aziridines

Published:2023 Issue:24 Volume:21 Page:4988-4992
ISSN:1477-0520
Container-title:Organic & Biomolecular Chemistry
language:en
Short-container-title:Org. Biomol. Chem.

Author:

Wang Nana¹,Du Youlong¹,Mei Haibo¹^ORCID,Escorihuela Jorge²^ORCID,Han Jianlin¹^ORCID

Affiliation:

1. Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China

2. Departamento de Química Orgánica, Universitat de València, Avda. Vicente Andrés Estellés s/n, Burjassot 46100, Valencia, Spain

Abstract

A Cu-promoted intramolecular cyclization of β-keto trifluoromethyl amines is developed, which provides the unprotected trifluoromethylated aziridines with good yields and excellent stereoselectivity.

Funder

National Natural Science Foundation of China

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Physical and Theoretical Chemistry,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/OB/D3OB00714F

Reference35 articles.

1. N-Trifluoromethyl Amines and Azoles: An Underexplored Functional Group in the Medicinal Chemist’s Toolbox

2. Substitution Effect of the Trifluoromethyl Group on the Bioactivity in Medicinal Chemistry: Statistical Analysis and Energy Calculations

3. Recent advances in the trifluoromethylation methodology and new CF3-containing drugs

4. Fluorine-containing drugs approved by the FDA in 2021

5. Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity

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