774607-93-1Relevant academic research and scientific papers
Improved synthesis of sterically encumbered heteroaromatic biaryls from aromatic β-keto esters
Rosen, Brandon R.,Ul Sharif, Ehesan,Miles, Dillon H.,Chan, Nicholas S.,Leleti, Manmohan R.,Powers, Jay P.
, (2020/03/25)
A protocol for the synthesis of hindered 4-aryl 2-aminopyrimidines from β–keto esters is described. The process employs trifluoroethanol as an essential additive to promote the guanidine condensation reaction, enabling the synthesis of 25 aryl- and heteroaryl substituted aminopyrimidines in good yields and high purities with no column chromatography. The conditions described herein are readily scalable and have been employed in the large-scale synthesis of the clinical A2a/A2bR antagonist AB928.
PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
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Page/Page column 80, (2012/02/03)
The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
Discovery of potent and selective pyrazolopyrimidine Janus kinase 2 inhibitors
Hanan, Emily J.,Van Abbema, Anne,Barrett, Kathy,Blair, Wade S.,Blaney, Jeff,Chang, Christine,Eigenbrot, Charles,Flynn, Sean,Gibbons, Paul,Hurley, Christopher A.,Kenny, Jane R.,Kulagowski, Janusz,Lee, Leslie,Magnuson, Steven R.,Morris, Claire,Murray, Jeremy,Pastor, Richard M.,Rawson, Tom,Siu, Michael,Ultsch, Mark,Zhou, Aihe,Sampath, Deepak,Lyssikatos, Joseph P.
, p. 10090 - 10107 (2013/01/16)
The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified the p
PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
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Page/Page column 117-118, (2010/05/14)
The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient. Ia
