Pyrazoles and pyrimidines have diverse biological and pharmacological activities. 269410-08-4, formula is C9H15BN2O2, Name is 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. There are a number of antimicrobial compounds containing pyrazole moiety as the core unit. Synthetic Route of 269410-08-4.
Ding, Li;Pannecouque, Christophe;De Clercq, Erik;Zhuang, Chunlin;Chen, Fen-Er research published 《 Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs》, the research content is summarized as follows. A series of novel heteroaromatic-difluoro-biphenyl-diarylpyrimidines were designed as non-nucleoside anti-HIV inhibitors targeting reverse transcriptase by a fragment-based replacement strategy with the purpose of improving the druggability. Hopping five- or six-membered heterocycle groups on the biphenyl moiety as bioisosterism for intrinsically cyanophenyl gave 23 derivatives All of these compounds possessed excellent HIV-1 inhibitory activity in the nanomolar range. Among them, 12g (I) with a 4-pyridine group displayed excellent inhibitory activity toward WT and mutant HIV virus possessing significant selectivity. Moreover, this compound exhibited a decent improvement in druggability than etravirine and rilpivirine: (1) The hydrochloric acid salt of 12g (I) exhibited significantly improved water solubility in different pH conditions. (2) 12g (I) did not show apparent CYP enzymic inhibitory activity or acute toxicity. (3) Excellent oral bioavailability was also revealed (F = 126%, rats) in 12g. Collectively, these novel heteroaromatic-biphenyl-DAPYs represent promising drug candidates for HIV clin. therapy.
269410-08-4, 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, also known as 4-Pyrazoleboronic acid pinacol ester , is a useful research compound. Its molecular formula is C9H15BN2O2 and its molecular weight is 194.04 g/mol. The purity is usually 95%.
4-Pyrazoleboronic acid pinacol ester is a useful reagent for Suzuki-Miyaura cross-couplings as well as Ruthenium-catalyzed asymmetric hydrogenation. 4-Pyrazoleboronic acid pinacol ester is also a useful reagent for preparing VEGF, Aurora, RHO (ROCK), Janus Kinase 2, c-MET, ALK, S-nitrsoflutathione reductase, CDC7, Acetyl-CoA carboxylase inhibitors.
4-Pyrazoleboronic acid pinacol ester is used in the preparation of Rho kinase (ROCK) inhibitors as wella s other biologically active compounds.
4-Pyrazoleboronic acid pinacol ester is an organic compound that is the product of a bifunctional coupling reaction between 4-pyrazolecarboxylic acid and pinacol. It has been shown to inhibit protein S6 kinase, which is involved in the regulation of cell growth and proliferation. This compound has also been shown to be effective against cancer cells, including those that are resistant to conventional chemotherapeutic drugs. 4-Pyrazoleboronic acid pinacol ester may also be used as a precursor for other compounds with pharmaceutical activity., Synthetic Route of 269410-08-4
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics