Piperidine, 1-[[3-(chloromethyl)phenyl]methyl]- synthesis

Yield:-

Reaction Conditions:

with thionyl chloride in dichloromethane at 0 - 30; for 3 h;Inert atmosphere;

Steps:

6.1 1-(3-(Chloromethyl)benzyl)piperidine 6b

Step 1
1-(3-(Chloromethyl)benzyl)piperidine 6b
3-(Piperidin-1-ylmethyl)phenylcarbinol 6a (1.7 g, 8.28 mmol, prepared according to the known method disclosed in "") was dissolved in 20 mL of dichloromethane, thionyl chloride (1.2 mL, 16.56 mmol) was added at 0°C, and the reaction solution was stirred at room temperature for 3 hours.
The reaction solution was concentrated under reduced pressure, added with saturated sodium carbonate solution (50 mL), and extracted with dichloromethane (100 mL*2).
The organic phases were combined, dried over anhydrous sodium sulfate and filtered.
The filtrate was concentrated under reduced pressure to obtain the crude title compound 6b (1.7 g), which was used directly in the next step without purification. MS m/z (ESI): 224.2 [M+1]

References:

EP3546457,2019,A1 Location in patent:Paragraph 0142; 0143