With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.62718-31-4,1-Benzylpiperidine-4-carbonitrile,as a common compound, the synthetic route is as follows.
62718-31-4, Benzylprotection of 1 to give 5 was achieved in 70-80% yield by reductive amination with benzaldehyde and sodium triacetoxyborohydride as the reducing agent in DCM as the solvent. Dehydration to the cyano compound 6 was performed under the same conditions as given for the preparation of 3. Subsequently, compound 6 was reacted with either benzylmagnesiumchloride or phenylmagnesiumchloride at rt overnight, followed by hydrolysis with 2M sulfuric acid to give the ketones 7 and 8, respectively, which were reductively aminated with benzylamine in ethanol in the presence of Pd/C (10%) at 3bar hydrogen pressure overnight in yields of 60-80% to the templates 9 and 10, respectively, which were used as racemates in the following synthetic steps. c) To a solution of l-benzyl-4-cyano-piperidine (9.3 g) in THF (90 ml) was added a solution of benzylmagnesiumchloride (1. 3 M in THF, 57 ml ; Fluka) at rt. Copper bromide was added (150 mg) and the reaction mixture was warmed to 60C for 8 h. The mixture was quenched by the addition of water (10 ml) and 15% sulfuric acid (65 ml) and stirring continued for 30 min. The THF was evaporated and 15% sodium hydroxide solution was added until the pH of the aqueous phase reached 8. The product was extracted with ether (2 x) to give crude material (10.8 g) which was purified by bulb-to-bulb destillation to give l- (l-benzyl- piperidin-4-yl)-2-phenyl-ethanone (5.1 g) as a colorless, viscous liquid.
62718-31-4 1-Benzylpiperidine-4-carbonitrile 793383, apiperidines compound, is more and more widely used in various fields.
Reference：
Patent; ACTELION PHARMACEUTICALS LTD; WO2004/2483; (2004); A1;,
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