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JOURNAL ARTICLE
RESEARCH SUPPORT, NON-U.S. GOV'T
En Route to 2-(Cyclobuten-1-yl)-3-(trifluoromethyl)-1H-indole.
Journal of Organic Chemistry 2018 Februrary 17
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.
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