En Route to 2-(Cyclobuten-1-yl)-3-(trifluoromethyl)-1H-indole

Autor: Marko Krivec, Martin Gazvoda, Janez Košmrlj, Zdenko Časar
Rok vydání: 2018
Předmět:
Zdroj: The Journal of Organic Chemistry. 83:2486-2493
ISSN: 1520-6904
0022-3263
DOI: 10.1021/acs.joc.8b00100
Popis: A six-step synthetic route from 4-chloro-2-methylaniline to 5-chloro-2-(cyclobut-1-en-1-yl)-3-(trifluoromethyl)-1H-indole (1) has been reported. Compound 1a is a key impurity of reverse transcriptase inhibitor efavirenz, an important anti-HIV/AIDS drug. Synthetic challenges, dead ends, and detours are discussed.
Databáze: OpenAIRE