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

Martin GazvodaMarko KrivecZdenko ČasarJanez Košmrlj

Published in: The Journal of organic chemistry (2018)

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.

Keyphrases

hiv aids
antiretroviral therapy
hiv infected
human immunodeficiency virus
hiv infected patients
adverse drug
drug induced