Uses
1-(4-Piperidinyl)ethanone is used in the synthesis of oral antagonists for the treatment of rheumatoid arthritis. Also used in the synthesis of p38 mitogen activated protein kinase.
Synthesis
General procedure for the synthesis of 1-(4-piperidinyl)ethanone hydrochloride from 1-N-BOC-4-acetylpiperidine: To an anhydrous dichloromethane (5 mL) solution of 1-N-BOC-4-acetylpiperidine (350 mg, 1.54 mmol) was slowly added a dioxane solution (2 mL) of 4 M HCl at 0 °C. The reaction mixture was stirred continuously at 0°C for 2 hours. Upon completion of the reaction, the mixture was concentrated by rotary evaporator to afford 1-(4-piperidinyl)ethanone hydrochloride (260 mg, 100% yield) as a white solid, which could be used directly in the subsequent reaction without further purification.
References
[1] Patent: WO2013/96744, 2013, A1. Location in patent: Page/Page column 192
[2] Patent: EP3255042, 2017, A2. Location in patent: Paragraph 0209; 0213