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azetidine-3,3-diyldimethanol synthesis

3synthesis methods
-

Yield:-

Reaction Conditions:

with hydrogen;palladium(II) hydroxide/carbon in methanol at 20;

Steps:

1

Azetidine-3,3-dimethanol hydrochloride (5). Pd(OH)2 (20% on C, 150 mg, 1.9 mmol) was added to a solution of 4 (400 mg, 1.9 mmol) in MeOH (4 mL) and left to stir under an atmosphere of hydrogen overnight at room temperature. The reaction was filtered through Celite and concentrated in vacuo. Chromatography (1 ,4-dioxane/NH4θH = 50:50) of the resulting residue afforded 5 as a colourless oil which was converted to its HCI salt (200 mg, 68%) for characterisation. 1H NMR (D2O): δ 3.97 (s, 4H), 3.69 (s, 4H). 13C NMR (D2O): δ 62.4, 49.8.

References:

WO2008/79028,2008,A1 Location in patent:Page/Page column 15-16