- METHOD FOR PRODUCING OPTICALLY ACTIVE 2, 3-BISPHOSPHINOPYRAZINE DERIVATIVE AND METHOD FOR PRODUCING OPTICALLY ACTIVE PHOSPHINE TRANSITION METAL COMPLEX
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In the method for producing an optically active 2,3-bisphosphinopyrazine derivative of the present invention, an optically active 2,3-bisphosphinopyrazine derivative represented by the following formula (3) is produced by the step of: preparing solution A containing 2,3-dihalogenopyrazine represented by the following formula (1) and a carboxylic acid amide coordinating solvent, lithiating an optically active R- or S-isomer of a hydrogen-phosphine borane compound represented by the following formula (2) to give a lithiated phosphine borane compound; adding solution B containing the lithiated phosphine borane compound to the solution A to perform an aromatic nucleophilic substitution reaction; and then performing a deboranation reaction. (For symbols in the formulas, see the description.)
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Paragraph 0085-0088
(2020/03/28)
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- PHOSPHINE TRANSITION METAL COMPLEX, METHOD FOR PRODUCING THE SAME AND ANTICANCER AGENT
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PROBLEM TO BE SOLVED: To provide a phosphine transition metal complex having excellent solubility to aqueous solvent, and higher anticancer activity than that of conventional cisplatin, and an anticancer agent including the same and a method for producing a phosphine transition metal complex using the same. SOLUTION: The present invention provides a phosphine transition metal complex represented by formula (1) (where R1-R4 and R6-R9 each denote an alkyl group, a cycloalkyl group, or an adamantyl group, R5 and R10 each denote a monovalent substituent, n and y each denote an integer of 0-4, M is a transition metal atom selected from gold, copper, silver). SELECTED DRAWING: None COPYRIGHT: (C)2020,JPO&INPIT
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Paragraph 0065
(2020/05/06)
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- METHOD FOR PRODUCING 2,3-BISPHOSPHINOPYRAZINE DERIVATIVE, AND METHOD FOR PRODUCING PHOSPHINE TRANSITION METAL COMPLEX
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There is provided a method for producing a 2,3-bisphosphinopyrazine derivative, the method comprising a first step of adding a base to a liquid comprising: 2,3-dihalogenopyrazine represented by the following general formula (1); a hydrogen-phosphine borane compound represented by the following general formula (2); and a deboranating agent, and allowing the resultant to react to thereby obtain the 2,3-bisphosphinopyrazine derivative represented by the following general formula (3). According to the present invention, a method for producing the industrially advantageous 2,3-bisphosphinopyrazine derivative can be provided.
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Paragraph 0094-0097
(2020/08/20)
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- Direct intramolecular carbon(sp2)-nitrogen(sp2) reductive elimination from gold(iii)
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The reactivity of bidentate AuIII-Cl species, [(C^N)AuCl2], with a bisphosphine or carbon donor ligands results in reductive elimination. Combined experimental and computational investigations lead to the first evidence of a direct intramolecular C(sp2)-N(sp2) bond formation from a monomeric [(C^N)AuCl2] gold(iii) complex. We show that bidentate ligated Au(iii) systems bypass transmetallation to form C(sp2)-N(sp2) species and NHC-Au-Cl. Mechanistic investigations of the reported transformation reveal a ligand-induced reductive elimination via a key AuIII intermediate. Kinetic studies of the reaction support a second-order rate process.
- Kim, Jong Hyun,Mertens, R. Tyler,Agarwal, Amal,Parkin, Sean,Berger, Gilles,Awuah, Samuel G.
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supporting information
p. 6273 - 6282
(2019/05/17)
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- Anticancer agent composition
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Provided is an anti-cancer agent composition exhibiting excellent solubility and exerting high anti-cancer activity while exhibiting low toxicity. An anti-cancer composition characterized by containing a cyclodextrin compound and a phosphine transition metal complex represented by general formula (1). (In the formula, R1 and R2 represent a linear or branched alkyl group, a cycloalkyl group, a cycloalkyl group having a substituent, an adamantyl group, a phenyl group, or a phenyl group having a substituent, have a carbon number between 1 and 10, and may represent the same group or different groups. R3 and R4 represent a hydrogen atom or a linear or branched alkyl group, have a carbon number between 1 and 6, and may represent the same group or different groups. R3 and R4 may form a saturated or unsaturated ring by bonding to one another and said saturated or unsaturated ring may have a substituent. M represents a transition metal atom selected from among gold, copper, and silver. X- represents an anion.)
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Paragraph 0099-0102
(2017/01/31)
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- ANTI-CANCER AGENT
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The anti-cancer agent of the present invention contains at least one kind of phosphine transition metal complex selected from a group of compounds represented by the following Formulae (1a) to (1d). According to this anti-cancer agent, an anti-cancer agent is provided which has a higher anti-cancer activity and lower toxicity compared to anti-cancer agents in the related art. In Formulae (1a), (1b), (1c), and (1d), R1 and R2 represent a linear or branched alkyl group, and R4 has a higher priority than R2 as ranked according to RS notation. R3 and R4 represent a hydrogen atom or a linear or branched alkyl group. M represents an atom of a transition metal selected from a group consisting of gold, copper, and silver. X? represents an anion.
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Page/Page column 6-7
(2012/10/08)
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- PHOSPHINE TRANSITION METAL COMPLEX, METHOD FOR PRODUCING THE SAME AND ANTITUMOR AGENT
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An anticancer agent having a novel chemical structure and high anticancer activity is provided. A phosphine transition metal complex of general formula (1) and an anticancer agent containing the complex are disclosed. R1 and R2, which may be the same or different, each represent a group having 1 to 10 carbon atoms selected from a straight-chain or branched alkyl group, a cycloalkyl group, a substituted cycloalkyl group, an adamantyl group, a phenyl group, and a substituted phenyl group; R3 and R4, which may be the same or different, each represent a hydrogen atom, a straight-chain alkyl group having 1 to 6 carbon atoms or branched alkyl group having 1 to 6 carbon atoms; or R3 and R4 are taken together to form a saturated or unsaturated ring which may have a substituted group; M represents a transition metal atom selected from the group consisting of gold, copper, and silver; and X- represents an anion.
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Page/Page column 9-10
(2009/04/23)
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