With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.214147-48-5,1-(4-Aminopiperidin-1-yl)ethanone hydrochloride,as a common compound, the synthetic route is as follows.
The sealed tube is charged with 7-bromo-5-chloroquinoxaline (50 mg; 0.21 mmol; 1.00 eq.), 1 -(4-aminopiperidin-1 -yl)ethan-1-one hydrochloride (38 mg; 0.27 mmol; 1.30 eq.), NaOtBu (59 mg; 0.62 mmol; 3.00 eqf.), BrettPhos Pd G1 (3.3 mg; 0.00 mmol; 0.02 eq.), BrettPhos (4.4 mg; 0.01 mmol; 0.04 eq.) and sealed with silicone PTFE coated cap. The air from the vessel is evacuated in vacuo thorough syringe and backfilled with argon. The cycle is repeated 3 times and anhydrous [1 ,4]-dioxane (1 .00 ml) is added thorough syringe. RM is heated and stirred for 1 h at 120C. Then RM is diluted with EtOAc and filtered through celite pad. Filtrate is evaporated resulted oily residue is purified by FCC (MeOH/DCM, gradient). 1-{4-[(8-Chloroquinoxalin- 6-yl)amino]piperidin-1-yl}ethan-1 -one (6.9 mg; 0.02 mmol; yield 10.4%;94% by UPLC) is obtained as brown glass.
214147-48-5, 214147-48-5 1-(4-Aminopiperidin-1-yl)ethanone hydrochloride 17221642, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; SELVITA S.A.; FABRITIUS, Charles-Henry Robert Yves; NOWAK, Mateusz Oktawian; WIKLIK, Katarzyna Anna; SABINIARZ, Aleksandra Barbara; BIE?, Marcin Dominik; BUDA, Anna Ma?gorzata; GUZIK, Pawel Szczepan; JAKUBIEC, Krzysztof Roman; MACIUSZEK, Monika; KWIECI?SKA, Katarzyna; TOMCZYK, Mateusz Micha?; GA??ZOWSKI, Micha? Miko?aj; GONDELA, Andrzej; DUDEK, ?ukasz Piotr; (681 pag.)WO2016/180536; (2016); A1;,
Piperidine – Wikipedia
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