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2-(3-PHENYL-[1,2,4]OXADIAZOL-5-YL)-ETHYLAMINE synthesis

2synthesis methods
-

Yield:805184-96-7 79%

Reaction Conditions:

with trifluoroacetic acid in dichloromethane at 20;

Steps:

Intermediate 1. 2-(3 -phenyl- 1 ,2,4-oxadiazol-5 -yl)ethanamine

Intermediate 1[00169] To a suspension of Intermediate 1A (1.2 g, 4.2 mmol) in DCM (1 1 mL) was added TFA (11 mL). The reaction mixture was stirred at rt for several hours. The reaction mixture was diluted with CH2CI2, and washed with saturated aHC03 then brine. The aqueous phases were extracted with CH2CI2 (3x), and the combined organic portions dried over Na2S04, filtered, and concentrated to give Intermediate 1(623 mg, 79% yield). HPLC/MS (Method C) retention time = 1.43 min, [M+H]+ 190.2 ; 1H NMR (500 MHz, chloroform-i/) (δ ppm): 1.63 (br s, 2 H), 3.09 (t, J=6.32 Hz, 2 H), 3.25 (t, J=6.32 Hz, 2 H), 7.46-7.53 (m, 3 H), 8.08 (d, J=6.05 Hz, 2 H).

References:

WO2013/48928,2013,A1 Location in patent:Paragraph 00169

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