Biarylhydrazine compounds and their adducts and applications in the preparation of antitumor drugs
The present invention discloses a biarylhydrazine compound and its application in the preparation of antitumor drugs, the structure of the arylhydrazine compound as shown in formula I, the adduct is a biarylhydrazine compound on the hydrazine group plus benzyloxycarbonyl glycyl prolyl. The anticancer activity of the biarylhydrazine compounds of the present invention is superior to that of the existing positive control drug procarbazine; its Z-GP adduct can significantly reduce in vitro toxicity and in vivo toxicity to normal cells, and can be excised by FΑP-α enzyme specific hydrolysis in vivo (Z-GP) to release hydrolysate products; its Z-GP adduct can significantly inhibit tumor growth in tumor-bearing nude mice and reduce toxicity to non-target organs.
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Paragraph 0058; 0064; 0065; 0131-0135
(2022/03/27)
Divergent Synthesis of 1H-Indazoles and 1H-Pyrazoles from Hydrazones via Iodine-Mediated Intramolecular Aryl and sp3 C–H Amination
A divergent intramolecular C–H amination of hydrazones has been developed employing molecular iodine (I2) as the sole oxidant. The required hydrazone substrates were readily obtained by condensation of hydrazines with the corresponding ketones.
Nickel-catalyzed N-arylation of benzophenone hydrazone with bromoarenes
A nickel-catalyzed method for the cross-coupling of benzophenone hydrazone with aryl bromides is described. The use of a simple Ni(ii)/NHC catalyst leads to the arylated hydrazones in good or acceptable yields. This protocol provides a simple, convenient alternative to the synthesis of arylhydrazines.
Tandem hydroformylation/Fischer indole synthesis: A novel and convenient approach to indoles from olefins
(Matrix presented) A novel one-pot synthesis of indole systems via tandem hydroformylation/Fischer indole synthesis starting from olefins and arylhydrazines is described. This tandem procedure leads directly to 3-substituted indoles if unsubstituted phenylhydrazine is used and to 3,5- respectively 3,7-disubstituted indoles if para- or ortho-substituted arylhydrazines are used.
Koehling, Petra,Schmidt, Axel M.,Eilbracht, Peter
p. 3213 - 3216
(2007/10/03)
A palladium-catalyzed method for the preparation of indoles via the Fischer indole synthesis
A Pd-catalyzed method for the preparation of N-aryl benzophenone hydrazones 4 is described. The use of a Pd/BINAP-based catalyst provides hydrazones 4 in good yields. Using 0.1 mol % of a Pd/9,9-dimethyl-4,5- bis(diphenylphosphino)xanthene (Xantphos) cata
Wagaw, Seble,Yang, Bryant H.,Buchwald, Stephen L.
p. 10251 - 10263
(2007/10/03)
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