89283-48-7Relevant academic research and scientific papers
BF3·SMe2 for Thiomethylation, Nitro Reduction and Tandem Reduction/SMe Insertion of Nitrogen Heterocycles
S?derstr?m, Marcus,Zamaratski, Edouard,Odell, Luke R.
, p. 5402 - 5408 (2019/06/27)
Herein, a general, solvent-free and straightforward thiomethylation of electron deficient heterocycles using BF3·SMe2 as a dual thiomethyl source and Lewis acidic activator is presented. A range of heterocycles including pyrimidine, pyrazine, pyridazine, thiazole and purine derivatives were successfully substituted using this method. An unexpected reductive property of BF3·SMe2 towards nitropyridines was also discovered including an intriguing tandem reduction/SMe insertion process in certain substrates. Notable features of the present work include its convenience and use of a non-malodorous reagent while the discovery of novel chemical transformations using BF3·SMe2 provides fundamental new insights into the reactivity of this commonly employed reagent.
Synthesis of Alkylated Pyrimidines via Photoinduced Coupling Using Benzophenone as a Mediator
Kamijo, Shin,Kamijo, Kaori,Murafuji, Toshihiro
, p. 2664 - 2671 (2017/03/14)
The synthesis of alkylated pyrimidines was achieved via benzophenone-mediated photoinduced coupling between saturated heterocycles and sulfonylpyrimidines. The pyrimidine ring was selectively introduced at the nonacidic C(sp3)-H bond proximal to heteroatoms including oxygen, nitrogen, and sulfur. This is a coupling reaction mediated solely by photoexcited benzophenone, an organic molecule, without the aid of any metallic catalysts or reagents.
INDOLE AND AZAINDOLE MODULATORS OF THE ALPHA 7 NACHR
-
Page/Page column 42-43, (2011/05/05)
This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a pharmaceutically acceptable salt thereof.
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 26-27, (2011/09/14)
The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R2, R3, R4 and R5 are defined in the summary of the invention), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
PYRAZOLO [1,5-a] PYRIMIDINES USEFUL AS JAK2 INHIBITORS
-
Page/Page column 64-65, (2009/08/14)
The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
Ledeboer, Mark W.,Pierce, Albert C.,Duffy, John P.,Gao, Huai,Messersmith, David,Salituro, Francesco G.,Nanthakumar, Suganthini,Come, Jon,Zuccola, Harmon J.,Swenson, Lora,Shlyakter, Dina,Mahajan, Sudipta,Hoock, Thomas,Fan, Bin,Tsai, Wan-Jung,Kolaczkowski, Elaine,Carrier, Scott,Hogan, James K.,Zessis, Richard,Pazhanisamy,Bennani, Youssef L.
scheme or table, p. 6529 - 6533 (2010/05/18)
Constitutive activation of the EPO/JAK2 signaling cascade has recently been implicated in a variety of myeloproliferative disorders including polycythemia vera, essential thrombocythemia and myelofibrosis. In an effort to uncover therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to discover selective inhibitors that block the kinase activity of JAK2. Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2.
PYRIMIDYL DERIVATIVES AS PROTEIN KINASE INHIBITORS
-
Page/Page column 46, (2008/12/06)
Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as w
[4,5']BIPYRIMIDINYL-6,4'-DIAMINE DERIVATIVES AS PROTEIN KINASE INHBITORS
-
Page/Page column 23, 30, 31, 60-61, (2008/06/13)
The invention provides a novel class of compounds of the Formula (I): in which the symbols have the meanings given in the description and claims, to pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prev
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 69, (2008/06/13)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 36, (2008/06/13)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di
