Aqueous phase synthesis, crystal structure and biological study of isoxazole extensions of pyrazole-4-carbaldehyde derivatives

作者：Wazalwar Sachin S; Banpurkar Anita R; Perdih Franc

来源：Journal of Molecular Structure, 2017, 1150: 258-267.

DOI：10.1016/j.molstruc.2017.08.094

• Aqueous phase synthesis
• One-pot synthesis
• Isoxazol derivatives
• 3-Methyl-4H-isoxazol-5-one
• 3-(substituted phenyl)-1-phenyl-1H-pyrazole-4-carbaldehyde

A series of novel isoxazol derivatives was synthesized by green route in aqueous phase at room temperature by the reaction of 3-methyl-4H-isoxazol-5-one with 3-(substituted phenyl)-1-phenyl-1H-pyrazole-4-carbaldehyde by one-pot Knoevenagel condensation method using sodium benzoate as a catalyst. Compounds were characterized on the basis of IR, H-1 NMR, mass spectroscopy and melting point determination. Crystal structures of five compounds were determined by X-ray diffraction. The compounds formed were screened for antibacterial and antifungal activity. Some compounds showed activity, close to ampicillin against E. coli, S. aureus, and S. pyogenus. Two compounds showed antifungal activity against C. albicans close to standard greseofulvin.

• 出版日期2017-12-15