Electric Literature of 201162-53-0, These common heterocyclic compound, 201162-53-0, name is 3-Boc-3,8-Diazabicyclo[3.2.1]octane, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Aldehyde Intermediate 2 (1.0 equiv) and /er/-butyl 3,8-diazabicyclo[3.2. l]octane-3- carboxylate (1.2 equiv) were combined into l,2-DCE (5 mL). To the mixture was added acetic acid (0.5 equiv). The mixture was stirred at rt for 3h. Solid NaBH(OAc)3(3.0 equiv) was then added into the reaction. The resulting mixture was stirred at rt overnight. The reaction was quenched with MeOH (10 mL) and washed with saturated NaHC03, water, and brine. The crude mixture was purified on a silica gel column to afford /er/-butyl 8-((2-ethyl-4′-(l,l,l,3,3,3-hexafluoro-2- hydroxypropan-2-yl)-[l,r-biphenyl]-4-yl)methyl)-3,8-diazabicyclo[3.2. l]octane-3-carboxylate (yield 55%) as a white solid.
The synthetic route of 201162-53-0 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ESCALIER BIOSCIENCES B.V.; MOHAN, Raju; NUSS, John; HARRIS, Jason; YUAN, Shendong; (144 pag.)WO2019/177996; (2019); A1;,
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