150187-64-7Relevant academic research and scientific papers
Nitrosation of derivatives of hydrazines, VIII: Novel oxidative C-N-coupling of indazoles and benzotriazoles with cyclic ethers
Hanefeld,Hartmann,Hunz
, p. 203 - 207 (1993)
Allopurinol, nitroindazoles and 5-nitrobenzotriazoles react with cyclic ethers under oxidation with nitrosyl-tetrafluoroborate or 2,3-dichloro-5,6-dicyanobenzoquinone yielding C-N-coupled products.
HETEROCYCLYLAMINO-SUBSTITUTED TRIAZOLES AS MODULATORS OF RHO-ASSOCIATED PROTEIN KINASE
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Page/Page column 87, (2019/08/12)
This invention relates to novel compounds and pharmaceutical compositions comprising. Compounds of the invention useful as modulators of Rho-associated protein kinase (ROCK), for example ROCK1 and/or ROCK2 inhibitors. Methods of treatment employing the compounds are also contemplated by the present invention. The compounds of the invention are useful in treating ROCK mediated diseases.
A mild and efficient THP protection of indazoles and benzyl alcohols in water
Zhan, Yang,Ding, Xiao,Wang, Hailong,Yu, Haihua,Ren, Feng
supporting information, p. 2150 - 2153 (2018/05/08)
A mild and efficient method for THP protection of indazoles and benzyl alcohols has been developed in water, the most environmentally friendly solvent, in which Tween 20 (2% w/w) was added to form aqueous micelles to increase the solubility of starting materials. This aqueous protocol allowed the reaction to proceed smoothly at room temperature and with only 1.2 equiv of DHP, providing moderate to good yields of THP protected products for a wide scope of substrates. In addition, the methodology was highly practical in the large-scale synthesis (1 g synthesis of 2c as an example), wherein the convenient work-up and purification procedure (simple filtration) made the protocol even more attractive.
PYRAZOLE DERIVATIVES AS P38 MAP INHIBITORS
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Paragraph 0550; 0551, (2015/07/27)
Compounds of formula (I): wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
PYRAZOLE DERIVATIVES AS P38 MAP INHIBITORS
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Page/Page column 68, (2014/03/25)
Compounds of formula (I) wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
Indazoles: Regioselective protection and subsequent amine coupling reactions
Slade, David J.,Pelz, Nicholas F.,Bodnar, Wanda,Lampe, John W.,Watson, Paul S.
supporting information; experimental part, p. 6331 - 6334 (2009/12/26)
(Chemical Equation Presented) Indazoles are unselectively protected under strongly basic conditions to give a mixture at N-1 and N-2. Under mildly acidic conditions, regioselective protection at N-2 takes place. Thermodynamic conditions lead to regioselective protection at N-1. This trend applies to various substituted indazoles. Protected 5-bromoindazoles participate in Buchwald reactions with a range of amines to generate novel derivatives.
