85738-39-2Relevant academic research and scientific papers
Structure-Activity Relationships of Pyrazolo[1,5- a]pyrimidin-7(4 H)-ones as Antitubercular Agents
Oh, Sangmi,Libardo, M. Daben J.,Azeeza, Shaik,Pauly, Gary T.,Roma, Jose Santinni O.,Sajid, Andaleeb,Tateishi, Yoshitaka,Duncombe, Caroline,Goodwin, Michael,Ioerger, Thomas R.,Wyatt, Paul G.,Ray, Peter C.,Gray, David W.,Boshoff, Helena I. M.,Barry, Clifton E.
, p. 479 - 492 (2021/01/26)
Pyrazolo[1,5-a]pyrimidin-7(4H)-one was identified through high-throughput whole-cell screening as a potential antituberculosis lead. The core of this scaffold has been identified several times previously and has been associated with various modes of actio
Design and evaluation of pyrazolopyrimidines as KCNQ channel modulators
Osuma, Augustine T.,Xu, Xiangdong,Wang, Zhi,Van Camp, Jennifer A.,Freiberg, Gail M.
, (2019/08/13)
Effective treatments of neuropathic pain have been a focus of many discovery programs. KCNQ (kv7) are voltage gated potassium channel openers that have the potential for the treatment of CNS disorders including neuropathic pain. Clinical studies have sugg
Synthesis of 4-substituted pyrazole-3,5-diamines: Via Suzuki-Miyaura coupling and iron-catalyzed reduction
Tomanová, Monika,Jedinák, Luká?,Ko?a?, Jan,Kvapil, Lubomír,Hradil, Pavel,Canka?, Petr
, p. 10200 - 10211 (2017/12/26)
A general and efficient synthesis of 4-substituted-1H-pyrazole-3,5-diamines was developed to access derivatives with an aryl, heteroaryl, or styryl group, which are otherwise relatively difficult to prepare. The first step is based on the Suzuki-Miyaura cross-coupling reaction utilizing the XPhos Pd G2 precatalyst. The coupling reactions of 4-bromo-3,5-dinitro-1H-pyrazole with the electron-rich/deficient or sterically demanding boronic acids enabled the production of the corresponding dinitropyrazoles. The subsequent iron-catalyzed reduction of both nitro groups with hydrazine hydrate accomplished the synthesis. The additional demethylation of the 4-methoxystyryl derivative allowed the production of the carboanalog of CAN508 reported as a selective CDK9 inhibitor.
A scalable approach to diaminopyrazoles using flow chemistry
Wilson, Noel S.,Osuma, Augustine T.,Camp, Jennifer A.Van,Xu, Xiangdong
scheme or table, p. 4498 - 4501 (2012/10/08)
This Letter reports on how the combination of microwave and continuous flow chemistry facilitated the convenient preparation of aminopyrazoles from commercial aryl halides. The method was applied to a variety of substrates with good to excellent yields an
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Page/Page column 39, (2012/11/08)
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
The Reaction of Phenylmalononitrile with Hydrazine. Synthesis and Properties of 3,5-Diamino-4-phenylpyrazole, 2-Amino-3-phenylpyrazolopyrimidine, and Related Compounds
Zvilichovsky, Gury,David, Mordechai
, p. 11 - 16 (2007/10/02)
3,5-Diamino-4-phenylpyrazole was prepared by the reaction of phenylmalononitrile with hydrazine hydrate.This hitherto unknown polyfunctional heterocycle reacted with acetylacetone, ethyl acetoacetate, 5-oxobutyraldehyde, malonaldehyde, diethyl (ethoxymeth
