- Oxidation of aromatic 1,2-dimethanols by activated dimethyl sulfoxide
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A series of substituted ortho-phthalaldehydes were prepared under mild conditions in respectable yields by oxidation of the corresponding dimethanols using oxalyl chloride activated dimethyl sulfoxide.
- Farooq
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Read Online
- Synthesis of benzobicycloheptanones via the trap of photogenerated ketene methide intermediate with olefins
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Irradiation of ortho-formyl dienes with UV light led to benzobicycloheptanones in high yields and chemoselectivities via a photogenerated ketene methide/Diels-Alder cascade reaction. The reaction mechanism was proposed to be a [1,5]-H shift process rather than a radical pathway based on control experiments. DFT calculations indicate that the energy of transition states is responsible for the high chemoselectivity observed in this protocol.
- Liu, Qiang,Meng, Jiang,Liu, Yang,Yang, Chao,Xia, Wujiong
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- Site-Selective Functionalization of (sp3)C?H Bonds Catalyzed by Artificial Metalloenzymes Containing an Iridium-Porphyrin Cofactor
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The selective functionalization of one C?H bond over others in nearly identical steric and electronic environments can facilitate the construction of complex molecules. We report site-selective functionalizations of C?H bonds, differentiated solely by rem
- Gu, Yang,Natoli, Sean N.,Liu, Zhennan,Clark, Douglas S.,Hartwig, John F.
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- IDO/TDO Inhibitor
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A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R1 and R2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R1 and R2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R4 represents, for example, —C(═NH)—HN2, and R6 represents, for example, a substituted or unsubstituted aryl group].
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Paragraph 0334-0336; 0368; 0369
(2020/08/19)
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- THIENODIAZEPINE DERIVATIVES AND APPLICATION THEREOF
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The present invention relates to a class of thienodiazepine derivatives and an application thereof in the preparation of a drug for the treatment of diseases associated with bromodomain and extra-terminal (BET) Bromodomain inhibitors. Specifically, the present invention relates to compounds represented by formulas (I) and (II), as well as pharmaceutically acceptable salts thereof.
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Paragraph 0270-0272
(2020/08/09)
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- Synthesis of 1,2-phenylenedimethanols by base-promoted reduction of isobenzofuran-1(3H)-ones with silane
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An efficient method for preparation of substituted 1,2-phenylenedimethanols and aliphatic 1,4-diols that are valuable intermediates in organic synthesis, has been developed by the base-promoted reduction of isobenzofuran-1(3H)-ones and γ-lactones with silane under mild conditions. Compared with traditional procedures using stoichiometric amounts of metal hydrides and alkyl reductants, the present method avoids the use of sensitive reagents and is operationally simple and a broad variety of functional groups are tolerated.
- Liu, Bin,Zhou, Xigeng
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supporting information
p. 725 - 728
(2018/12/11)
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- Cobalt-Catalyzed Formal [4+2] Cycloaddition of α,α′-Dichloro-ortho-Xylenes with Alkynes
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A formal [4+2] cycloaddition of α,α′-dichloro-ortho-xylenes with various alkynes has been developed using a low-valent cobalt catalyst. The transformation has a wide substrate scope and high functional-group tolerance and led to 1,4-dihydronaphthalenes. T
- Komeyama, Kimihiro,Okamoto, Yuji,Takaki, Ken
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supporting information
p. 11325 - 11328
(2016/02/19)
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- Design, synthesis and discovery of 1-(2-(6-chloro-3-methylsulfonyl)- naphthyl)-1H-pyrazole-5-carboxylamides as highly potent factor Xa inhibitors
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Based upon the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides reported in our previous communications, we designed and discovered 2-(6-chloro-3-methylsulfonyl)-naphthyl as an optimal factor Xa S1 binding element. Employing a key Diels-Alder reaction of 1,4-dihydro-2,3-benzoxathiin-3- oxide with maleic anhydride and a key Cu(I)-mediated methylsulfonylation, we prepared two biphenyl 1-(2-(6-chloro-3-methylsulfonyl)-naphthyl)-1H-pyrazole-5- carboxylamides as highly potent factor Xa inhibitors with Ki values of 0.065 nM and 0.045 nM respectively, and demonstrated the synergistically enhanced binding interaction in the factor Xa S1 site.
- Jia, Zhaozhong Jon,Scarborough, Robert Murry,Zhang, Penglie,Halfon, Sherin,Arfsten, Ann Elizabeth,Sinha, Uma,Zhu, Bing-Yan
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scheme or table
p. 1004 - 1007
(2010/03/31)
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- SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS
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The present invention relates to A compound of the formula Ia wherein in any of its stereoisomers forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.
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Page/Page column 205-206
(2009/01/24)
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- 2,4-DIAMINOQUINAZOLINES FOR SPINAL MUSCULAR ATROPHY
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2,4-Diaminoquinazolines of formulae I-IV and VI (I, II, III, IV and VI) are useful for treating spinal muscular atrophy (SMA).
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Page/Page column 63
(2010/02/15)
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- Azabicyclic compounds for the treatment of disease
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The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1-2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1-2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which α7 is known to be involved.
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- 2-[2H-(1,3-dihydroisoindole)alkylene]-4,5-dihydroimidazoles and pharmaceutical compositions thereof
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A compound of formula (I): STR1 or a pharmaceutically acceptable salt, ester or amide thereof, wherein: Z represents a residue of a substituted or unsubstituted aryl group, X represents O or NRo wherein Ro represents a hydrogen atom,
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- Potential GABAB Receptor Antagonists. III Folded Baclofen Analogues Based on Phthalide
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Possible analogues of baclofen, 3-aminomethyl-5-chloro-, 3-aminomethyl-6-chloro- and 3-aminomethyl-5,6-dichloro-isobenzofuran-1(3H)-one, have been prepared for evaluation as antispasticity agents.The corresponding 3-hydroxyisobenzofuran-1(3H)-one was reac
- Donati, Cosimo,Prager, Rolf H.,Weber, Ben
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p. 787 - 795
(2007/10/02)
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