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3-(Azetidin-3-yloxy)-benzonitrile synthesis

2synthesis methods
1-Azetidinecarboxylic acid, 3-(3-cyanophenoxy)-, 1,1-dimethylethyl ester

1350362-24-1
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3-(Azetidin-3-yloxy)-benzonitrile

954223-73-5
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Yield:954223-73-5 262.3 mg

Reaction Conditions:

with trifluoroacetic acid in dichloromethane at 20; for 2 h;

Steps:

1.1.4.2 1 .4.2 Synthesis of 3-(azetidin-3-yloxy)benzonitrile a1 -45.

Trifluoroacetic acid (10 ml) is added to a solution of tert-butyl 3-(3- cyanophenoxy)azetidine-1-carboxylate a1 -43 (260 mg, 0.95 mmol, 1 eq) in dichloromethane (10 ml). The reaction mixture is stirred for 2 hours at room temperature, then concentrated to dryness to afford 262.3 mg of crude 3-(azetidin-3- yloxy)benzonitrile a1 -45 as an oil. This oil is used in the next step without any further purification.Yield: 100%. LC-MS (MH+): 175.

References:

WO2013/53725,2013,A1 Location in patent:Page/Page column 40-41