575452-22-1Relevant academic research and scientific papers
4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS
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Paragraph 00366, (2016/06/28)
Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3 and R4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
Synthesis of substituted-3-iodo-1H-pyrazole derivatives and their further modification under Sonogashira cross-coupling reaction conditions
Mazeikaite, Rita,Sudzius, Jurgis,Urbelis, Gintaras,Labanauskas, Linas
, p. 54 - 71 (2014/12/10)
A convenient synthetic route for preparation of valuable synthetic intermediates - 1-(1-ethoxyethyl)-3-iodo-1H-pyrazole derivatives has been developed. During this work protection reaction of N-H bond in substituted 3-iodo-1H-pyrazole derivatives with ethyl vinyl ether and migration of ethoxyethyl protecting group was investigated. Synthetic possibilities of Sonogashira cross-coupling reactions of substituted 1-(1-ethoxyethyl)-3-iodo-1H-pyrazole derivatives with phenylacetylene were studied and evaluated.
Highly hydrophobic isoreticular porous metal-organic frameworks for the capture of harmful volatile organic compounds
Padial, Natalia M.,Quartapelle Procopio, Elsa,Montoro, Carmen,Lopez, Elena,Oltra, J. Enrique,Colombo, Valentina,Maspero, Angelo,Masciocchi, Norberto,Galli, Simona,Senkovska, Irena,Kaskel, Stefan,Barea, Elisa,Navarro, Jorge A. R.
supporting information, p. 8290 - 8294 (2013/09/02)
Tunable hydrophobicity: Efficient air filters for the protection against chemical warfare agents might be achieved by surface functionalization of the pores in robust metal-organic frameworks (MOFs) with fluoroalkyl residues and the precise control of their pore size (see picture). These MOFs capture harmful volatile organic compounds even under extremely moist conditions (80 % relative humidity). Copyright
Improved synthesis of 1H-pyrazole-4-carbaldehyde
Taydakov, Ilya V.,Krasnoselskiy, Sergey S.,Dutova, Tatiana Y.
experimental part, p. 2430 - 2434 (2011/08/05)
A simple and convenient two-step method for the synthesis of the title compound 1 was developed using N-protected 4-pyrazolilmagnesium bromide 9 as a key intermediate. Laborious procedures for purification or isolation of target compound are not required, therefore, up to 20g of 1 could be obtained in a single run.
PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS
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Page/Page column 104, (2010/08/07)
The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.
ANTIFUNGAL TRIAZOLE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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, (2010/04/23)
The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against vario
Enantioselective synthesis of janus kinase inhibitor INCB018424 via an organocatalytic aza-michael reaction
Lin, Qiyan,Meloni, David,Pan, Yongchun,Xia, Michael,Rodgers, James,Shepard, Stacey,Li, Mei,Galya, Laurine,Metcalf, Brian,Yue, Tai-N,Liu, Pingli,Zhou, Jiacheng
supporting information; experimental part, p. 1999 - 2002 (2009/09/06)
An enantioselective synthesis of INCB018424 via organocatalytic asymmetric aza-Michael addition of pyrazoles (16 or 20) to (E)-3- cyclopentylacrylaldehyde (23) using diarylprolinol silyl ether as the catalyst was developed. Michael adducts (R)-24 and (R)-27 were isolated in good yield and high ee and were readily converted to INCB018424.
ANTIFUNGAL TRIAZOLE DERIVATIVES, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Page/Page column 21-22, (2008/12/07)
The present invention relates to triazole derivaties, a method for the preparation thereof, and a pharmaceutical composition containing the same as an active ingredient. The inventive triazole derivaties have an excellent antifungal activity against vario
A multifunctional high-spin biradical pyrazolylbipyridine- bisnitronylnitroxide
Zoppellaro, Giorgio,Enkelmann, Volker,Geies, Ahmed,Baumgarten, Martin
, p. 4929 - 4932 (2007/10/03)
(Chemical Equation Presented) Synthesis and UV-vis, IR, and EPR spectroscopic characterizations, together with X-ray structural analysis, of functional nitronyl- and iminonitroxides attached to pyrazolylbipyridine are described. The exchange interactions between the nitronylnitroxides are found to be stronger than for the iminonitroxides. Although the substitution of a pyridine with the pyrazole ring leads to shorter distances and larger dipolar couplings, the exchange interaction is diminished. While compound 1 forms dimers in the solid state, the terpyridine 3 leads to supramolecular π-stacking.
Ethyl vinyl ether - An agent for protection of the pyrazole NH-fragment. A convenient method for the preparation of N-unsubstituted 4-alkynylpyrazoles
Vasilevsky, Sergei F.,Klyatskaya, Svetlana V.,Tretyakov, Eugene V.,Elguero, José
, p. 879 - 886 (2007/10/03)
N-Unsubstituted 4-iodopyrazole (1) is easily converted into 4-alkynyl derivatives (5) in moderate to good overall yields by using intermediate protection of the nitrogen atom of the pyrazole ring by ethyl vinyl ether.
