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Green synthesis and antifungal activities of novel 3‐(trifluoromethyl)‐4, 5‐dihydro‐1 H ‐furo[2,3‐ c ]pyrazole derivatives
Author(s) -
Tan Fangshun,
Su Shennan,
Liu Zhenzhong
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3998
Subject(s) - chemistry , pyrazole , trifluoromethyl , pyrazolones , antifungal , solvent , organic chemistry , combinatorial chemistry , medicine , alkyl , dermatology
Trifluoromethylated molecules, as well as pyrazol‐3‐one derivatives, are found in a wide range of biologically active compounds. An highly facile, green and mild access to substituted 3‐(trifluoromethyl)‐4,5‐dihydro‐1 H ‐furo[2,3‐ c ]pyrazole derivatives by the cascade [3 + 2] Michael/Alkylation of unsaturated pyrazolones with α‐bromomalonate has been developed. The reactions can be performed in a easily available and environmentally benign solvent, and the substituted 3‐(trifluoromethyl)‐4,5‐dihydro‐1 H ‐furo[2,3‐ c ]pyrazole derivatives can be obtained in good to excellent yields by a simple purification step. The antifungal activities of these functional pyrazole derivatives were also evaluated and they showed high antifungal activity against Alternaria solani .