Downstream synthetic route of 52763-21-0

52763-21-0 Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride 2723880, apiperidines compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.52763-21-0,Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride,as a common compound, the synthetic route is as follows.

Preparation 29: Ethyl 1-benzyl-3-oxo-4-(prop-2-en-1-yl)piperidine-4-carboxylate (P29)A mixture of potassium ferf-butoxide (3.77 g, 33. 58 mmol) in THF (100 m L) was stirred at RT for 0.5 h. The resulting milky solution was cooled to 0 C, and then Ethyl l-benzyl-3-oxopiperidine-4-carboxylate hydrochloride (5 g, 16.79 mmol) was added portion wise keeping the internal temperature below 5 C. The mixture was then warmed to RT and further stirred for 1 h, resulting in a yellow solution. After cooling to 0 C, allyl bromide (1.6 mL, 18.47 mmol) was added dropwise. The reaction mixture was warmed to RT and stirred overnight. The reaction solution was cooled to 0 C, and 50 m L of saturated N H4CI solution was added. After extraction and phase separation, the aqueous phase was extracted twice with 100 mL of EA. The combined organic phases were washed with 100 m L of saturated NaCI solution and dried; the solvent was evaporated under reduced pressure and the obtained crude material was purified by FC on silica gel (eluent: Cy to Cy/AcOEt 80/20) to give ethyl l-benzyl-3-oxo-4-(prop-2-en- l-yl)piperidine-4-carboxylate (p29, 4.23 g, y= 84%) as a yellow oil.MS (ES) (m/z): 302.23 [M+H]+., 52763-21-0

52763-21-0 Ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloride 2723880, apiperidines compound, is more and more widely used in various fields.

Reference£º
Patent; SHIRE INTERNATIONAL GMBH; SEMERARO, Teresa; TARSI, Luca; MICHELI, Fabrizio; LUKER, Tim; CREMONESI, Susanna; (122 pag.)WO2016/42451; (2016); A1;,
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