3-(2-methylphenyl)piperidine synthesis

Yield: 93.9%

Reaction Conditions:

with palladium diacetate;C₃H₆BNO₂ in tetrahydrofuran at 60; for 24 h;Schlenk technique;Inert atmosphere;

Steps:

10 Example 10: Preparation of 3-(2-methylphenyl)piperidine
Weigh β-alanine (222.8mg, 2.5mmol) and addShrek tube,Under the protection of inert gas,Cool to 0°C,Add the tetrahydrofuran complex of borane (1M, 5.0mmol),Stir the reaction at room temperature for 24h,The oxazoborane obtained by evacuating the solvent under vacuum was used directly in the next step.Add in the Shrek tube with oxazoborane still under the protection of inert gas3-(2-methylphenyl)pyridine (71.5mg, 0.5mmol),Tetrahydrofuran (2.0mL),Palladium acetate (11.3 mg, 0.05 mmol).The reaction was stirred at 60°C for 24h.The resulting reactant was purified by silica gel column (dichloromethane/methanol) to obtain3-(2-methylphenyl)piperidine (82.3mg) yield 93.9%

References:

CN112707857, 2021, A Location in patent:Paragraph 0067; 0068; 0069; 0070; 0071