- Synthesis of symmetrical dinitro-and diamino-substituted Troeger's base analogues
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This report describes a new synthetic approach to symmetrical diamino-substituted Troeger's base analogues, allowing the synthesis of 1,7-, and 4,10-diamino derivatives with no additional substituents and of 3,9-diamino derivative with methyl groups in the 1-, 4-, 7-and 10-positions. The synthesis uses regioselective nitration of dihalo-substituted-or tetrahalo-substituted Troeger's bases followed either by hydrogenation of the nitro functions accompanied by removal of halogen atoms or alternatively by chemoselective reduction of nitro groups to obtain the dihalo-diamino- substituted Troeger's base analogues. The 2,8-diamino derivatives, not accessible by this approach, can be prepared by Buchwald-Hartwig amination of the 2,8-dibromo-substituted Troeger's bases.
- Sturala, Jiri,Cibulka, Radek
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- 4,5,6-TRI-SUBSTITUTED INDAZOLES DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof
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- GPR40 RECEPTOR AGONIST, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.
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Paragraph 1400-1403
(2014/05/24)
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- TETRACYCLIC COMPOUND
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Provided are a tetracyclic compound represented by the formula (I): [in the formula(I),the formula (A) represents a benzene ring or the like, X represents CH or a nitrogen atom, Q represents -O- or the like, R1, R2, and R3 may be the same or different and each represent a hydrogen atom or the like, 1, m, and n each represent an integer from one to the maximum substitutable number of substituents, and R4 and R5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.
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- The oxidative bromination and iodination of dimethylacetanilides
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The oxidative bromination and iodination of the six dimethylacetanilides have been examined; whereas bromination of 2,4-dimethyl- and 2,6-dimethylacetanilides using potassium bromide, sodium tungstate and peracetic acid gave predominantly the 6- and 4-bro
- Medina, Inmaculada C. Rodriguez,Hanson, James R.
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p. 428 - 429
(2007/10/03)
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- Halogenation Using Quaternary Ammonium Polyhalides. XI. Bromination of Acetanilides by Use of Tetraalkylammonium Polyhalides
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The reaction of acetanilides with tetraalkylammonium polyhalides, such as tetrabutylammonium tribromide, benzyltrimethylammonium tribromide, and benzyltrimethylammonium chlorobromate(1-), in dichloromethane-methanol at room temperature gave bromosubstituted acetanilides in good yields, respectively.
- Kajigaeshi, Shoji,Kakinami, Takaaki,Yamasaki, Hiromichi,Fujisaki, Shizuo,Okamoto, Tsuyoshi
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p. 2681 - 2683
(2007/10/02)
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