497064-60-5Relevant articles and documents
Biarylhydrazine compounds and their adducts and applications in the preparation of antitumor drugs
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Paragraph 0058; 0068; 0069; 0082; 0083, (2022/03/27)
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.
CuI/4-hydro-L-proline as a more effective catalytic system for coupling of aryl bromides with N-boc hydrazine and aqueous ammonia
Jiang, Liqin,Lu, Xu,Zhang, Hui,Jiang, Yongwen,Ma, Dawei
experimental part, p. 4542 - 4546 (2009/09/25)
(Chemical Equation Presented) CuI/4-hydroxy-L-proline-catalyzed coupling of aryl bromides and N-Boc hydrazine takes place in DMSO at 80°C to give N-aryl hydrazides. When aryl iodides are employed, this reaction completes at 50°C and no ligand is required. Under the catalysis of CuI/4-hydroxy-L- proline, the coupling reaction of aqueous ammonia with aryl bromides proceeds smoothly at 50°C to afford primary arylamines. In this case K 2CO3 is found as a better base than Cs2CO 3. These processes allow assembly of N-aryl hydrazides and primary arylamines that bear a wide range of functional groups including hydroxyl, amine, trifluoromethyl, ester, nitro, and ketone.
