26956-09-2Relevant articles and documents
ISOQUINOLINES AS INHIBITORS OF HPK1
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Paragraph 2546; 2547, (2018/10/21)
Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.
Tuning azoheteroarene photoswitch performance through heteroaryl design
Calbo, Joaquín,Weston, Claire E.,White, Andrew J. P.,Rzepa, Henry S.,Contreras-García, Julia,Fuchter, Matthew J.
supporting information, p. 1261 - 1274 (2017/05/15)
Photoswitchable compounds, which can be reversibly switched between two isomers by light, continue to attract significant attention for a wide array of applications. Azoheteroarenes represent a relatively new but understudied type of photoswitch, where one of the aryl rings from the conventional azobenzene class has been replaced with a fivemembered heteroaromatic ring. Initial studies have suggested the azoheteroarenes-the arylazopyrazoles in particular- to have excellent photoswitching properties (quantitative switching and long Z isomer half-life). Here we present a systematic computational and experimental study to elucidate the origin of the long thermal half-lives and excellent addressability of the arylazopyrazoles, and apply this understanding to determine important structure-property relationships for a wide array of comparable azoheteroaryl photoswitches. We identify compounds with Z isomer half-lives ranging from seconds to hours, to days and to years, and variable absorption characteristics, all through tuning of the heteraromatic ring. Conformation perhaps plays the largest role in determining such properties: the compounds with the longest isomerization half-lives adopt a T-shaped ground state Z isomer conformation and proceed through a T-shaped isomerization pathway, whereas the most complete photoswitching is achieved for compounds that have a twisted (rather than T-shaped) Z isomer conformation. By balancing these factors, we report a new azopyrazole 3pzH, which can be quantitatively switched to its Z isomer (1/2 = 74 d at 25 °C). Given the large tunability of their properties, the predictive nature of their performance, and the other functional opportunities afforded by usage of a heteroaromatic system, we believe the azoheteroaryl photoswitches to have huge potential in a wide range of optically addressable applications.
Faujasite catalyzed nitrodeiodination of iodopyrazoles
Ravi,Tewari, Surya P.
, p. 35 - 39 (2013/09/12)
Nitrodeiodination of iodopyrazoles using nitric acid/Faujasite has been investigated. The present procedure is simple, rapid and convenient and requires no sulfuric acid or oleum and may be applied for the synthesis of several nitropyrazoles in good yield
A simple and environmentally benign nitration of pyrazoles by impregnated bismuth nitrate
Ravi,Gore, Girish M.,Tewari, Surya P.,Sikder, Arun K.
, p. 1322 - 1327 (2014/01/06)
We report herein a facile, rapid, and environmentally friendly synthesis of nitropyrazoles in good yields using silica-bismuth nitrate and silica-sulfuric acid-bismuth nitrate at room temperature for the first time. The relatively non-toxic nature, ease o
Silica-sulfuric acid catalyzed nitrodeiodination of iodopyrazoles
Ravi,Gore, Girish M.,Sikder, Arun K.,Tewari, Surya P.
experimental part, p. 3463 - 3471 (2012/09/22)
We report here the synthesis of nitropyrazoles in good to excellent yields from iodopyrazoles over silica-sulfuric acid catalyst for the first time. The present procedure require less acid, offers a simplified workup procedure, and may be applied for the
Facile and environmentally friendly synthesis of nitropyrazoles using montmorillonite K-10 impregnated with bismuth nitrate
Ravi,Tewari, Surya P.
experimental part, p. 37 - 41 (2012/04/10)
Nitropyrazoles in higher yields were synthesized using montmorillonite K-10 impregnated with bismuth nitrate and the present procedure may be applied for the nitration of a wide variety of azoles in the drug and pharmaceutical industries.
