- A new efficient synthesis of pyrazoles from hydrazonoyl halides and β-oxophosphonates
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A new practical and efficient synthesis of 1,3,5-trisubstituted pyrazoles has been developed by reacting of hydrazonoyl halides with β-oxophosphonates under mild conditions in good yields with excellent regioselectivity. This process employs an addition-elimination sequence. Wide scope, functional group compatibility has been established.
- Sun, Aixue,Ye, Jia-Hai,Yu, Haitao,Zhang, Wenchao,Wang, Xiaolong
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supporting information
p. 889 - 892
(2015/03/03)
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- A new efficient synthesis of pyrazoles from hydrazonoyl halides and β-oxophosphonates
-
A new practical and efficient synthesis of 1,3,5-trisubstituted pyrazoles has been developed by reacting of hydrazonoyl halides with β- oxophosphonates under mild conditions in good yields with excellent regioselectivity. This process employs an addition-elimination sequence. Wide scope, functional group compatibility has been established.
- Sun, Aixue,Ye, Jia-Hai,Yu, Haitao,Zhang, Wenchao,Wang, Xiaolong
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supporting information
p. 889 - 892
(2014/02/14)
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- Synthesis, central and peripheral benzodiazepine receptor affinity of pyrazole and pyrazole-containing polycyclic derivatives
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A series of new pyrazole-condensed 6,5,5 tricyclic compounds were synthesized and tested to evaluate their binding affinities at both central (CBR) and peripheral (PBR) benzodiazepine receptors. Some 1-aryl-5- phenylpyrazole derivatives were also prepared and tested for comparison with their corresponding rigid tricyclic analogs. Among the newly synthesized 1-aryl-1,4-dihydro-indeno[1,2-c]pyrazoles bearing both an ethoxycarbonyl group at position 3 and a carbonyl function at the position 4, compound 4b emerged as a new potent (IC50 = 26.4 nM) and selective CBR ligand. The 4-oxo-1-aryl-1,4-dihydro-indeno[1,2-c]pyrazole diethylamide derivative 14a was instead identified as a relatively potent (IC50 = 124 nM) but highly selective PBR ligand.
- Campagna, Francesco,Palluotto, Fausta,Carotti, Angelo,Maciocco, Elisabetta
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p. 849 - 856
(2007/10/03)
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