- A synthetic approach to chrysophaentin F
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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.
- Vendeville, Jean-Baptiste,Matters, Rebecca F.,Chen, Anqi,Light, Mark E.,Tizzard, Graham J.,Chai, Christina L. L.,Harrowven, David C.
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supporting information
p. 4837 - 4840
(2019/05/02)
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- Palladium-catalyzed three-component coupling reactions of 2-(cyanomethyl)phenol, aryl halides, and carbon monoxide
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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.
- Murai, Masahito,Okamoto, Kazuhiro,Miki, Koji,Ohe, Kouichi
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supporting information
p. 4432 - 4437
(2015/06/08)
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- HISTONE DEMETHYLASE INHIBITORS
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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.
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Paragraph 00730; 00731
(2014/06/24)
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- Water-promoted ortho-selective monohydroxymethylation of phenols in the NaBO2 system
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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.
- Li, Hui-Jing,Wu, Ying-Ying,Wu, Qin-Xi,Wang, Rui,Dai, Chun-Yang,Shen, Zhi-Lun,Xie, Cheng-Long,Wu, Yan-Chao
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p. 3100 - 3107
(2014/05/06)
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- PYRAZOLE COMPOUNDS ACTING AGAINST ALLERGIC, INFLAMMATORY AND IMMUNE DISORDERS
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The present invention relates to pyrazole amide derivatives pharmaceutical compositions containing these compounds and to their use in therapy.
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Page/Page column 41
(2012/05/05)
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- PYRAZOLE AND TRIAZOLE CARBOXAMIDES AS CRAC CHANNEL INHIBITORS
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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.
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Page/Page column 44-45
(2010/11/05)
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- N-PYRAZOLYL CARBOXAMIDES AS CRAC CHANNEL INHIBITORS
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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.
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Page/Page column 52
(2010/11/05)
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- A convenient method to reduce hydroxyl-substituted aromatic carboxylic acid with NaBH4/Me2SO4/B(OMe)3
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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.
- Zhou, Yuhan,Gao, Guchao,Li, Hui,Qu, Jingping
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p. 3260 - 3263
(2008/09/20)
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- NOVEL 1 -BENZYL-4-PIPERIDINAMINES THAT ARE USEFUL IN THE TREATMENT OF COPD AND ASTHMA
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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
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Page/Page column 34
(2010/11/27)
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- Combinational therapy involving a small molecule inhibitor of the MDM2: P53 interaction
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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.
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Page/Page column 51
(2008/06/13)
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- Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity
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The disruption of the p53-Hdm2 protein-protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione scaffold as a suitable template for inhibiting this interaction by binding to the Hdm2 protein. Several compounds have been made with improved potency, solubility, and cell-based activities.
- Leonard, Kristi,Marugan, Juan Jose,Raboisson, Pierre,Calvo, Raul,Gushue, Joan M.,Koblish, Holly K.,Lattanze, Jennifer,Zhao, Shuyuan,Cummings, Maxwell D.,Player, Mark R.,Maroney, Anna C.,Lu, Tianbao
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p. 3463 - 3468
(2007/10/03)
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- Efficient and selective reduction protocols of the 2,2-dimethyl-1,3- benzodioxan-4-one functional group to readily provide both substituted salicylaldehydes and 2-hydroxybenzyl alcohols
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Two complementary procedures have been developed that selectively allow for the synthesis of either substituted salicylaldehydes or the corresponding 2-hydroxylbenzyl alcohols upon treatment of the 2,2-dimethyl-1,3-benzodioxan-4- one functional group with DIBAL-H or LAH, respectively.
- Bajwa, Naval,Jennings, Michael P.
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p. 3646 - 3649
(2007/10/03)
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- Discovery of new chemical leads for selective EP1 receptor antagonists
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A series of 4-({2-[alkyl(phenylsulfonyl)amino]phenoxy}methyl)benzoic acids were identified as functional PGE2 antagonists with selectivity for the EP1 receptor subtype starting from a chemical lead 1, which was found while screening our in-house compound library. Discovery of the optimized analogs 21-23 is presented here and structure-activity relationships (SAR) are also discussed.
- Naganawa, Atsushi,Saito, Tetsuji,Nagao, Yuuki,Egashira, Hiromu,Iwahashi, Maki,Kambe, Tohru,Koketsu, Masatoshi,Yamamoto, Hiroshi,Kobayashi, Michiyoshi,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Kondo, Kigen,Toda, Masaaki
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p. 5562 - 5577
(2007/10/03)
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- Substituted 1,4-diazepines and uses thereof
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The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and R3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino; or R3—X— is hydrogen or an electron pair; R4 is oxygen or —NR9R10; R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
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- WATER-SOLUBLE SHPS AS NOVEL ALKYLATING AGENTS
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The present invention relates to compounds according to the structure (I): Where R is —CH3 or —CH2CH2Cl; R′ is C1-C7 alkyl or —CH2CH2Cl; R2 or R4 is OPOsub
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- Sulfonamide and carboxamide derivatives and drugs containing the same as the active ingredient
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The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1is —COR1, —CH═CH—COR1/
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- DIPHENYLETHANE COMPOUNDS CONTAINING A SATURATED HETEROCYCLIC GROUP, THEIR PREPARATION, AND THEIR THERAPEUTIC USE
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Compounds of formula (I): STR1 wherein: R 1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R 2a, R 2b, R 2c, R 3a, R. sup.3b, R. sup.3c and R 3d are hydrogen or various other groups or
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