64917-81-3Relevant academic research and scientific papers
A synthetic approach to chrysophaentin F
Vendeville, Jean-Baptiste,Matters, Rebecca F.,Chen, Anqi,Light, Mark E.,Tizzard, Graham J.,Chai, Christina L. L.,Harrowven, David C.
supporting information, p. 4837 - 4840 (2019/05/02)
The chrysophaentins are a newly discovered natural product family displaying promising anti-infective activity. Herein we describe an approach to chrysophaentin F that uses an array of metal catalysed coupling reactions (Cu, Ni, Pd, W, Mo) to form key bonds.
Palladium-catalyzed three-component coupling reactions of 2-(cyanomethyl)phenol, aryl halides, and carbon monoxide
Murai, Masahito,Okamoto, Kazuhiro,Miki, Koji,Ohe, Kouichi
supporting information, p. 4432 - 4437 (2015/06/08)
Three-component coupling reactions of 2-(cyanomethyl)phenol, aryl halides, and carbon monoxide (CO) in orthogonal-tandem catalysis were investigated. In the reactions, 2-(cyanomethyl)phenyl esters, which are produced through Pd(PPh3)4-catalyzed alkoxycarbonylation of aryl halides with 2-(cyanomethyl)phenol, undergo cycloisomerization in situ catalyzed by Pd(PCy3)2 as a co-catalyst to give 3-acyl-2-aminobenzofurans. Palladium species with homoleptic tertiary phosphines, such as Pd(PPh3)4 and Pd(PCy3)2, can catalyze the mechanistically distinct reactions in an orthogonal-tandem manner without interference. By switching the base used in this reaction, 3-acyl-2-(N-acylamino)benzofurans were obtained as major products instead of 3-acyl-2-aminobenzofurans. Given that 2-(cyanomethyl)phenols can be synthesized from commercially available salicylic acid derivatives in two steps, the present method thus provides facile access to synthetically useful 3-acyl-2-aminobenzofurans.
HISTONE DEMETHYLASE INHIBITORS
-
Paragraph 00730; 00731, (2014/06/24)
Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. 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.
Water-promoted ortho-selective monohydroxymethylation of phenols in the NaBO2 system
Li, Hui-Jing,Wu, Ying-Ying,Wu, Qin-Xi,Wang, Rui,Dai, Chun-Yang,Shen, Zhi-Lun,Xie, Cheng-Long,Wu, Yan-Chao
, p. 3100 - 3107 (2014/05/06)
Water-promoted ortho-selective monohydroxymethylation of phenols in the NaBO2 system generates salicyl alcohols in 65-97% yields. A remarkable rate-enhancement by water was observed, and NaBO2 appeared to serve the dual role of a suitable base and an efficient chelating reagent. This protocol possesses many advantages such as short reaction times, expanded substrate scope, and high mono- and regio-selectivities. The experimental results were explained by the calculations based on local ionisation energy minima, leading to a possible reaction mechanism.
PYRAZOLE COMPOUNDS ACTING AGAINST ALLERGIC, INFLAMMATORY AND IMMUNE DISORDERS
-
Page/Page column 41, (2012/05/05)
The present invention relates to pyrazole amide derivatives pharmaceutical compositions containing these compounds and to their use in therapy.
PYRAZOLE AND TRIAZOLE CARBOXAMIDES AS CRAC CHANNEL INHIBITORS
-
Page/Page column 44-45, (2010/11/05)
The present invention relates to amide compounds of formula (I) processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing these compounds and to their use in therapy.
N-PYRAZOLYL CARBOXAMIDES AS CRAC CHANNEL INHIBITORS
-
Page/Page column 52, (2010/11/05)
The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.
A convenient method to reduce hydroxyl-substituted aromatic carboxylic acid with NaBH4/Me2SO4/B(OMe)3
Zhou, Yuhan,Gao, Guchao,Li, Hui,Qu, Jingping
, p. 3260 - 3263 (2008/09/20)
The reduction of hydroxyl-substituted aromatic carboxylic acid with NaBH4/Me2SO4/B(OMe)3 is described. Borane is generated by the reaction of NaBH4 with Me2SO4 in THF, which is as efficient as the commercial one. B(OMe)3 has been successfully applied to increase the reactivity and selectivity of this reaction. The optimum ratio of borane/B(OMe)3/acid is studied, and a variety of hydroxyl-substituted aromatic acids are reduced in good yields.
NOVEL 1 -BENZYL-4-PIPERIDINAMINES THAT ARE USEFUL IN THE TREATMENT OF COPD AND ASTHMA
-
Page/Page column 34, (2010/11/27)
The invention provides 1 -benzyl- 4 -piperidinamines of the general formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory diseses such a
Combinational therapy involving a small molecule inhibitor of the MDM2: P53 interaction
-
Page/Page column 51, (2008/06/13)
The present invention is directed to a combinational therapy for treating cancer or other cell proliferative diseases. Such a therapy combines the use of radiation therapy or chemotherapy with the use of a small molecule inhibitor of the MDM2: p53 interaction.
