760-81-6Relevant academic research and scientific papers
BICYCLIC COMPOUNDS AS PESTICIDES
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, (2019/10/17)
The present application relates to novel bicyclic compounds, to compositions comprising these compounds, to the use thereof for control of animal pests and to processes and intermediates for the preparation thereof.
Regioselective rapid analogue syntheses of 1-methyl-3,5-diarylpyrazoles via palladium-catalysed coupling to 3(5)-pyrazolyl nonaflates
Bourrain, Sylvie,Ridgill, Mark,Collins, Ian
, p. 795 - 798 (2007/10/03)
Regioselective rapid analogue syntheses of 1-methyl-3,5-diarylpyrazoles were developed, based on Pd-catalysed couplings to 1-methyl-3(5)-arylpyrazole nonaflates, which offered an advantage in hydrolytic stability over the corresponding triflates. The new bifunctional reagent 1-methyl-3-bromo-pyrazol- 5-yl nonaflate underwent highly chemoselective Pd-catalysed couplings to the nonaflate, followed by Suzuki couplings to the bromide, allowing sequential, regioselective introduction of the two aryl substituents.
Synthesis and antitumor activity of methyltriazene prodrugs simultaneously releasing DNA-methylating agents and the antiresistance drug O 6-benzylguanine
Wanner, Martin J.,Koch, Melle,Koomen, Gerrit-Jan
, p. 6875 - 6883 (2007/10/03)
Active resistance of tumor cells against DNA alkylating agents arises by the production of high levels of the DNA repair protein O6- alkylguanine-DNA alkyltransferase (AGT). This resistance during treatment with, for example, the anticancer agent temozolomide can be reversed by administration of O6-benzylguanine, a purine that transfers its benzyl group to AGT and irreversibly inactivates it. Stimulated by the favorable therapeutic properties of temozolomide we designed and synthesized DNA-methylating triazenes built on the anti-resistance benzylguanine ring system. The condensation reaction between 2-nitrosopurines and acylhydrazines proved to be very suitable to prepare acylated methyltriazenes. Fine-tuning of the release rate of both the methylating agent (diazomethane) and of O6-benzylguanine was accomplished by variation of the hydrolysis-sensitive acyl substituent in 5. Hydrolysis studies were performed with 1H NMR and revealed that the p-nitrophenyl substituted triazene 26 showed an optimal hydrolysis rate (t 1/2 = 23 min) and almost 100% selectivity for the desired fragmentation route. In vitro antitumor studies in the 60 human tumor cell line panel of the National Cancer Institute confirmed the superior properties ofp-nitrophenyl-protected methyl triazene 26, showing mean IC50 values of 10 μM. compared to 100 μM for temozolomide. In analogy with temozolomide, triazene 26 showed however low preference for each of the cancer subpanels, with IC50 values between 8 and 14 μM.
Triazolone derivatives, use thereof, and intermediates therefor
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, (2008/06/13)
Triazolone derivatives represented by the formula wherein R1represents optionally substituted C1-10alkyl, A1—L1—, A1—ON═CA2, etc.; R2represents hydrogen, C1-6alkyl, etc.; R3represents C1-6alkoxy, etc.; one of T, U, and V represents CR4, another represents CH or nitrogen, and the remaining one represents CR5or nitrogen; and W represents CR6or nitrogen.
Peptide carbazates
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, (2008/06/13)
Certain novel peptide carbazates, their preparation, pharmaceutical compositions and novel methods of treating pancreatitis.
