- 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; 0508; 0509
(2020/08/19)
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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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- 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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supporting information
p. 13954 - 13960
(2019/08/30)
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- Catalytic Electrophilic Alkylation of p-Quinones through a Redox Chain Reaction
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Allylation and benzylation of p-quinones was achieved through an unusual redox chain reaction. Mechanistic studies suggest that the existence of trace hydroquinone initiates a redox chain reaction that consists of a Lewis acid catalyzed Friedel–Crafts alkylation and a subsequent redox equilibrium that regenerates hydroquinone. The electrophiles could be various allylic and benzylic esters. The addition of Hantzsch ester as an initiator improves the efficiency of the reaction.
- Xu, Xiao-Long,Li, Zhi
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supporting information
p. 8196 - 8200
(2017/06/30)
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- 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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p. 8143 - 8155
(2015/03/18)
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- 7-Methoxy-3-nitro-2-naphthalenemethanol - A new phototrigger for caging applications
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Synthesis, photochemistry and photorelease properties of 7-methoxy-3-nitro-2-naphthalenemethanol (MNNM) are described. Photoirradiation (≥370 nm) of MNNM covalently linked to hippuric acid causes efficient release (~90%) of hippuric acid.
- Singh, Anil K.,Khade, Prashant K.
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p. 4899 - 4902
(2011/10/05)
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- Photoexcited proton transfer from enhanced photoacids
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Naphthols with electron-withdrawing groups such as cyano or methanesulfonyl at C-5 and C-8 exhibit greatly enhanced photoacidity. This increase in photoacidity enables the substituted naphthols to undergo excited-state proton transfer (ESPT) in alcohols and Me2SO in the absence of water. In aqueous tetrahydrofuran solution, efficient proton transfer to water occurs at much lower water concentrations than with the parent naphthol, and the kinetics of proton transfer indicate that a smaller water cluster is involved.
- Tolbert, Laren M.,Haubrich, Jeanne E.
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p. 10593 - 10600
(2007/10/02)
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- A synthesis of two novel benzo[f]ninhydrin analogs: 6-methoxybenzo[f]ninhydrin and thieno[f]ninhydrin
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Improved methodology for the synthesis of benzo[f]ninhydrin (1) is described. The generality of this approach is illustrated with the synthesis of two novel analogs, 6-methoxybenzo[f]ninhydrin (3) and thieno[f]ninhydrin (4).
- Heffner,Joullie
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p. 1055 - 1069
(2007/10/02)
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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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