A New, One-Pot, Multicomponent Synthesis of Bioactive N -Pyrazolylformamidines under Microwave Irradiation
A one-pot, three-component, microwave-assisted reaction of polysubstituted 5-aminopyrazoles, triethyl orthoformate, and a series of cyclic secondary amines was developed and successfully employed for the synthesis of novel N-pyrazolylformamidines. Under catalyst-free conditions, the reaction proceed...
| Main Authors: | , , |
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| Format: | Journal Article |
| Published: |
Georg Thieme Verlag
2016
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| Online Access: | http://hdl.handle.net/20.500.11937/24652 |
| Summary: | A one-pot, three-component, microwave-assisted reaction of polysubstituted 5-aminopyrazoles, triethyl orthoformate, and a series of cyclic secondary amines was developed and successfully employed for the synthesis of novel N-pyrazolylformamidines. Under catalyst-free conditions, the reaction proceeded in a chemo- and regioselective manner, resulting in the formation of unsymmetric formamidines, which were isolated in high yields and purity. Some of the prepared compounds were found to inhibit interleukin-17 secretion in phenotypic in vitro assays. |
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