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The general synthesis procedure of phenyl-isoxazole–Carboxamide derivatives (2a-2f)

MH Mohammed Hawash
NJ Nidal Jaradat
AE Ahmad M. Eid
AA Ahmad Abubaker
OM Ola Mufleh
QA Qusay Al-Hroub
SS Shorooq Sobuh
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The 5-(methyl)-3-phenyl-1,2-isoxazole-4–Carboxylic acid (compound 1) (609.60 mg, 3 mmol) was dissolved in 20 ml of dichloromethane (DCM), followed by the addition of di methylamino-pyridine (DMAP; 73.30 mg, 0.6 mmol), and N′-ethyl carbodiimide hydrochloride (EDC; 632.61 mg, 3.30 mmol). Then the mixture was stirred under argon inert gas at room temperature for 30 min, and the aniline derivatives (3.2 mmol) were added. The reactions were monitored by thin-layer chromatography (TLC). After that, the solvent was removed under vacuum pressure and dissolved again in DCM, then extracted with HCl (2 N) to remove any excess aniline derivatives. The organic layer was dried over Na2SO4 and evaporated under reduced pressure. The obtained final products were purified by flash chromatography using the convenient solvent systems (DCM: ethyl acetate and/or n-hexane: ethyl acetate) and/or then purified by recrystallization utilizing the convenient solvent system [18].

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