87486-35-9Relevant academic research and scientific papers
INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
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, (2016/04/26)
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Scalable synthesis of functionalised 2-pyridones via [4+2] cycloaddition reactions of 2-pyrazinones and alkynylboronates
Harker, Wesley R.R.,Delaney, Patrick M.,Simms, Michael,Tozer, Matthew J.,Harrity, Joseph P.A.
, p. 1546 - 1552 (2013/02/25)
The multigram synthesis of N-protected 2-pyridone boronic acid derivatives via a [4+2] cycloaddition of alkynylboronates with 2-pyrazinones is presented. The reactions are highly chemoselective, and generally highly regioselective although trimethylsilyl-substituted alkynylboronates have proven to be an exception. Nonetheless, in this latter case, separation of regioisomers was successfully accomplished via high performance counter-current chromatography allowing isolation of analytically pure 2-pyridones. Further derivatisations of trimethylsilyl-substituted 2-pyridone boronates were performed providing access to a selection of functionalised scaffolds.
SUBSTITUTED OXAZOLIDINONES AND THEIR USE
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Page/Page column 46, (2010/12/29)
The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases
Intramolecular Diels-Alder synthesis of 7-aza-α-carboline compounds
Wallace, Michael B.,Scorah, Nicholas,Vu, Phong H.,Brown, Jason W.,Stafford, Jeffrey A.,Dong, Qing
supporting information; experimental part, p. 1739 - 1741 (2010/05/18)
An efficient, versatile, and scalable route for the synthesis of 7-aza-α-carboline compounds is described. The tricyclic system has been prepared from modified pyrazinones using a key intramolecular [4+2] Diels-Alder transformation.
Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives
Francois, Isabelle E.J.A.,Cammue, Bruno P.A.,Bresseleers, Sara,Fleuren, Hein,Hoornaert, Georges,Mehta, Vaibhav P.,Modha, Sachin G.,Van der Eycken, Erik V.,Thevissen, Karin
supporting information; experimental part, p. 4064 - 4066 (2010/03/25)
We synthesized a family of 3,5-dichloropyrazin-2(1H)-one derivatives and assessed their in vitro fungicidal activity against Candida albicans. Compounds 11 and 20 were most active against C. albicans and induced accumulation of reactive oxygen species in
Design and synthesis of novel type VI-like β-turn mimetics. Diversity at the i+1 and the i+2 position
De Borggraeve, Wim M.,Verbist, Bie M.P.,Rombouts, Frederik J.R.,Pawar, Vijaykumar G.,Smets, Wim J.,Kamoune, Laila,Alen, Jo,Van Der Eycken, Erik V.,Compernolle, Frans,Hoornaert, Georges J.
, p. 11597 - 11612 (2007/10/03)
In this paper, a synthetic approach for functionalised 5-aminopiperidinone- 2-carboxylate (APC) systems as non-pro cis-peptide bond containing external β-turn mimics is presented. The scope and limitations of the synthetic method are discussed and the pot
A new synthesis of substituted 2(1H)-pyrazinones
Vekemans,Pollers Wieers,Hoornaert
, p. 919 - 923 (2007/10/02)
The hydrohalides of 2-sec-aminoalkanenitriles on treatment with oxalyl halides in o-dichlorobenzene at 80-100° give 3,5-dihalo-2(1H)-pyrazinones, of which the 3-halo substituent is easily replaced by nucleophiles. A reaction mechanism for the pyrazinone s
