With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.479195-19-2,2-Oxa-8-azaspiro[4.5]decane hydrochloride,as a common compound, the synthetic route is as follows.
To a solution 2-oxa-8-azaspiro[4.5]decane, HC1 (1 g, 5.63 mmol) and DIEA (2.9 mL, 16.9 mmol) in anhydrous CH3CN (35 mL) was added isopropyl 2-(5-bromo-4- chloro-2,6-dimethylpyridin-3-yl)-2-oxoacetate (1.9 g, 5.63 mmol) at rt. The resulting mixture was placed in a pre-heated oil bath (80 C) and stirred for 18 h; cooled, and concentrated. The crude product was charged (DCM) to a 80 g ISCO silica gel cartridge and gradient elution (5 – 35% EtOAc/hexanes) using an Isolera chromatography station to give isopropyl 2-(5-bromo-2,6-dimethyl-4-(2-oxa-8-azaspiro[4.5]decan-8-yl)pyridin-3- yl)-2-oxoacetate 990 mg (40%). 1H NMR (500 MHz, CDC13) delta 5.08-5.05 (m, 1H), 3.75 (t, J=7.3 Hz, 2H), 3.37 (s, 2H), 3.36-3.34 (m, 4H), 2.61 (s, 3H), 2.30 (s, 3H), 1.73-1.71 (m, 2H), 1.50 (br. s, 4H), 1.29 (d, J=6.2 Hz, 6H). UPLC (M+H) = 441.1.
479195-19-2, 479195-19-2 2-Oxa-8-azaspiro[4.5]decane hydrochloride 21955264, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; VIIV HEALTHCARE UK (NO.5) LIMITED; KADOW, John F.; NAIDU, B. Narasimhulu; ROMINE, Jeffrey Lee; SIVAPRAKASAM, Prasanna; ST. LAURENT, Denis R.; (204 pag.)WO2017/25864; (2017); A1;,
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