19064-18-7Relevant articles and documents
Preparation method of 2, 6-difluorobenzyl alcohol
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Paragraph 0027-0069, (2021/11/10)
The invention discloses a preparation method of 2, 6-difluorobenzyl alcohol. By adding a phase transfer catalyst, a reduction reaction can be carried out in two phases, and the yield of the reduction reaction can be obviously improved. Part of NaBH4 is dissolved in advance, and the rest NaBH4 is added in batches subsequently, so that the reduction efficiency of the NaBH4 is improved, and the purpose of improving the yield of the reduction reaction is finally achieved. By adding a Lewis acid catalyst, the reduction reaction yield can be effectively improved, the purity of 2, 6-difluorobenzyl alcohol is improved, and the residual amount of methyl 2, 6-difluorobenzoate is reduced.
Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency
Bollini, Mariela,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Tirado-Rives, Julian,Anderson, Karen S.,Jorgensen, William L.
, p. 1110 - 1113 (2013/03/14)
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved activity towards Tyr181Cys containing variants was pursued with the assistance of free energy perturbation (FEP) calculations. Optimization of the 4-R substituent in 1 led to ethyl and isopropyl analogs 1e and 1f with 1-7 nM potency towards both the wild-type virus and a Tyr181C variant.