Downstream synthetic route of 7006-50-0

7006-50-0 4-(Methylamino)-1-benzylpiperidine 4136128, 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.7006-50-0,4-(Methylamino)-1-benzylpiperidine,as a common compound, the synthetic route is as follows.,7006-50-0

Preparation 21; N-(1-Benzy(piperidin-4-yl)-N-methyipyridin-2-amine A mixture of 4-methylamino-1-benzylpiperidine; [(1.5g, 6.2mmol), J. Med. Chem. 39, 3769-89; 1996] 1-bromopyridine (0.98g, 6.2mmol), sodium tert-butoxide (0.68g, 7.3mmol), 1,3-bis(diphenylphosphino)propane (102mg, 0.24mmol) and tris (dibenzylideneacetone)dipalladium(O) (113mg, 0.12mmol) in toluene (20mL) was heated under reflux for 4 hours. Tlc analysis showed that there was still starting material present and so further bromopyridine (0.49g, 3.1 mmol), tris (dibenzylideneacetone)dipalladium(0) (113mg, 0.12mmol), bis(diphenylphosphino)propane (102mg, 0.24mmol) and sodium tert-butoxide (0.68g, 7.3mmol) were added and heating continued for a further 3 hours. The mixture was then diluted with dichloromethane and washed with brine. The organic solution was dried over magnesium sulfate and concentrated in vacuo and the residue was purified by column chromatography on silica gel, eluting with dichloromethane: methanol: 0. 88 ammonia, 90: 10:1 to afford the title compound in 40% yield, 0.69g.

7006-50-0 4-(Methylamino)-1-benzylpiperidine 4136128, apiperidines compound, is more and more widely used in various fields.

Reference:
Patent; PFIZER LIMITED; PFIZER INC.; WO2005/105779; (2005); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem