A series of N-aryl and N-heteroaryl pyrazoles have been deproto-metallated using a 2,2,6,6-tetramethylpiperidino-based mixed lithium-zinc combination. Mono-, di-, and tri-iodides have been obtained after subsequent trapping with iodine, depending on the substrate and on the quantity of base used. The results have been discussed in the light of the CH acidities of the substrates, determined both...

The synthesis under MW irradiation without solvent of 19 pyrazoles, of which only 8 were known, is described. They bear C-methyl groups and trityl, diphenylmethyl and benzyl groups at positions 1 and 4 of the pyrazole ring. In the reaction between pyrazole and trityl bromide an unexpected reaction occurred and 4-(9-phenyl-9H-fluoren-9-yl)-1Hpyrazole (7) was isolated.

Synthesis of novel pyrazole-fused heterocycles, i.e., dihydro-1Hor 2H-oxepino[3,2c]pyrazoles (6 or 7) from 4-allyloxy-1H-pyrazoles (1) via combination of Claisen rearrangement and ring-closing metathesis (RCM) has been achieved. A suitable catalyst for the RCM of 5-allyl-4allyloxy-1H-pyrazoles (4) was proved to be the Grubbs second generation catalyst (Grubbs2nd) to give the predicted RCM produ...

To develop compounds that are antagonists on ER , but not ER , we have added basic side-chains typically found in nonsteroidal antiestrogens to pyrazole compounds that bind with much higher affinity to ER than to ER . In this way we have developed basic side-chain pyrazoles (BSC-pyrazoles) that are high affinity, potent, selective antagonists on ER . These BSCpyrazoles are themselves inactive o...

Easy accessible isoxazol-5(4 H )-ones are useful precursors of heterocycles. In this context we report the ruthenium-catalyzed transformation 4-alkenyl-substituted isoxazol-5-ones to afford 1 -pyrrole derivatives. The operative conditions were proven be effective also on cyclohexane-fused isoxazolones giving 4,5,6,7-tetrahydroindoles. Reactions, which allow access tri-and tetra-substituted pyrr...

The cyclin-dependent kinase inhibitor, CAN508, was protected with di-tert-butyl dicarbonate to access the amino-benzoylated pyrazoles. The bromo derivatives were further arylated by Suzuki-Miyaura coupling using the XPhos Pd G2 pre-catalyst. The coupling reaction provided generally the para-substituted benzoylpyrazoles in the higher yields than the meta-substituted ones. The Boc groups were onl...

The title mol-ecule, C35H25N3O, is a tri-phenyl-amine derivative with the 4-position substituted by an aldehyde group, and the 4'-position substituted by a 6-phenyl-2,2'-bi-pyridine group. The whole mol-ecule is non-planar and the dihedral angle between the core benzene and pyridine rings is 36.96 (5)°. The dihedral angle between the phenyl and benzaldehyde groups bonded to the amine N atom is ...

The reaction of P-diketones 1 with phenyl hydrazine afforded 5-aryl-3-(1- methyl-5-nitro-2-imidazoly1)-1-phenylpyrazole (2) and 3-aryl-5-(1-methyl-5- nitro-2-imidazoly1) -1-phenylpyrazole (3). The reaction of diketones (1) with urea in the presence of p-toluenesulfonic acid gave 4-(or 6-)aryl-6-(or 4-)(1-methyl- 5-nitro-2-imidazolyl)-1-(lH)pyrimidones (4). The structures of all compounds w...