(2S)-2-(broMoMethyl)-1-Methyl-Pyrrolidine synthesis

Yield:60365-88-0 21.99%

Reaction Conditions:

with carbon tetrabromide;triphenylphosphine in dichloromethane at 0 - 20; for 1 h;

Steps:

10

To a solution of the (S)-(1-methylpyrrolidin-2-yl) methanol (500 mg, 4.341 mmol) in methylene chloride (10 mL) was added triphenylphosphine (1.48 g, 5.644 mmol) followed by careful addition of carbon tetrabromide (1.87 g, 5.644 mmol) at 0⁰C. The reaction mixture was allowed to stir for 1 hour at room temperature. Water was added and the organic layer was washed with brine, dried over sodium sulfate and the solvent was removed in vacuo. The resulting oil was purified by silica gel chromatography (1:3 hexanes/ethyl acetate). Bromide as a clear oil (170 mg, 21.99%, clear oil).

References:

WO2022/87371,2022,A1 Location in patent:Paragraph 0188