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474527-76-9

1-Pyrrolidineethanol,3-methyl-,(3R)-(9CI) synthesis

5synthesis methods
-

Yield:474527-76-9 30%

Reaction Conditions:

with potassium carbonate in acetonitrile; for 48 h;Reflux;

Steps:

1 (R)-2-(3-Methylpyrrolidin-l-yl)ethanol (4')

(R)-2-(3-Methylpyrrolidin-l-yl)ethanol (4') [00124] To a solution of V (4.5 g, 19 mmol) in acetonitrile (200 mL) and potassium carbonate (5.5 g, 30.5 mmol) is added ethanolamine (1.2 mL, 19 mmol) and the resulting suspension is heated at reflux for 48 hours. The cooled solution is filtered and concentrated. This residue is dissolved in DCM (100 mL) and washed with 5% aqueous sodium hydroxide (2 x 50 mL), brine, dried over anhydrous sodium sulfate, filtered, and concentrated to yield a pale yellow oil. This oil is distilled (100-110, 3 mm Hg) to yield 4 as a clear colorless oil (1.4 g, 30% yield).

References:

WO2013/90921,2013,A1 Location in patent:Paragraph 00124