With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.169447-70-5,(S)-tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
A 100 mL round-bottom flask was charged with 2-chloro-4-(morpholin-4- yl)benzaldehyde (0.800 g, 3.54 mmol, 1.00 equiv), tert-butyl (2S)-2-methylpiperazine-l- carboxylate (0.783 g, 3.91 mmol, 1.10 equiv) , 1,2-dichloroethane (20 mL). The mixture was stirred for 30 min at room temperature. Sodium triacetoxyborohydride (2.26 g, 10.7 mmol, 3.00 equiv) was added. The resulting solution was stirred overnight at room temperature, diluted with ]0 (30 mL), extracted with dichloromethane (3 x 30 mL) and the organic layers were combined, dried over Na2S04, filtered and concentrated under reduced pressure. The residue was chromatographed on a silia gel column with ethyl acetate/petroleum ether (25/75) to provide 1.20 g (74% yield) of tert-butyl (2S)-4-[[2-chloro-4-(morpholin-4- yl)phenyl]methyl]-2-methylpiperazine-l-carboxylate as a white solid. LCMS (ESI, m/z): 410 [M+H]+., 169447-70-5
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Reference£º
Patent; ABIDE THERAPEUTICS; THE SCRIPPS RESEARCH INSTITUTE; CISAR, Justin, S.; GRICE, Chery, A.; JONES, Todd, K.; NIPHAKIS, Micah, J.; CHANG, Jae, Won; LUM, Kenneth, M.; CRAVATT, Benjamin, F.; WO2013/103973; (2013); A1;,
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