- Preparation method of aza compounds
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The invention discloses a preparation method of aza compounds N-((5-(3-hydroxyphenyl)-2H-1,2,4-triazole-3-ol)methyl)-N-propyl-1-amine. 3-(3-hydroxyphenyl)ethyl acrylate serves as an initial material, a target product 7 is obtained through reduction, acyla
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Paragraph 0024-0026
(2017/07/20)
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- COMPOSITIONS FOR THE TREATMENT OF KIDNEY AND/OR LIVER DISEASE
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The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of kidney and/or liver disease.
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- Benzocarbazoles dioxane derivatives, its preparation process and its use in medicine
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The invention relates to a benzodioxane derivative, a preparation method thereof and application of the derivative in medicines. Specifically, the invention relates to a novel benzodioxane derivative shown as a formula (I), medial salt thereof or a medicine composition containing the derivative, and a preparation method of the derivative. The invention further relates to a use of the benzodioxane derivative and the medial salt thereof or the medicine composition containing the derivative in preparing therapeutic agent, especially GPR 40 agonist, and a drug for treating the diseases such as diabetes, metabolic disorders and the like, wherein each substituent group in the formula (I) is as defined in the description.
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- Chemo- and Regioselective Hydrogenolysis of Diaryl Ether C-O Bonds by a Robust Heterogeneous Ni/C Catalyst: Applications to the Cleavage of Complex Lignin-Related Fragments
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We report the chemo- and regioselective hydrogenolysis of the C-O bonds in di-ortho-substituted diaryl ethers under the catalysis of a supported nickel catalyst. The catalyst comprises heterogeneous nickel particles supported on activated carbon and furnishes arenes and phenols in high yields without hydrogenation. The high thermal stability of the embedded metal particles allows C-O bond cleavage to occur in highly substituted diaryl ether units akin to those in lignin. Preliminary mechanistic experiments show that this catalyst undergoes sintering less readily than previously reported catalyst particles that form from a solution of [Ni(cod)2].
- Gao, Fang,Webb, Jonathan D.,Hartwig, John F.
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p. 1474 - 1478
(2016/02/12)
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- Calcilytic compounds
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Novel calcilytic compounds and methods of using them are provided.
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Page/Page column 11; 24
(2016/01/25)
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- Development of a practical and scalable synthesis of a potent CRTH2 antagonist
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This contribution describes the process research and development of a practical and scalable synthetic method towards compound 1, which has a potent CRTH2 antagonistic activity. The medicinal chemistry synthetic route and second generation synthetic route
- Yoshida, Shinya,Yoshino, Toshitaka,Miyafuji, Akio,Yasuda, Hironobu,Kimura, Takenori,Takahashi, Takumi,Mukuta, Takashi
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p. 1544 - 1551
(2013/02/23)
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- POLYCYCLIC ACID COMPOUNDS USEFUL AS CRTH2 ANTAGONISTS AND ANTIALLERGIC AGENTS
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The present invention relates to a novel compound or a salt thereof, which is useful as a CRTH2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bronchitis, food allergy, inflammation of the nasal sinuses, multiple sclerosis, angiitis, or chronic obstructive pulmonary disease (COPD) and the like.
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Page/Page column 110
(2008/12/06)
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- Identification and synthesis of a novel selective partial PPARδ agonist with full efficacy on lipid metabolism in vitro and in vivo
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The aim was to identify a novel selective PPARδ agonist with full efficacy on free fatty acid (FFA) oxidation in vitro and plasma lipid correction in vivo. Using the triple PPARα,γ,δ agonist 1 as the structural starting point, we wanted to investigate the
- Sauerberg, Per,Olsen, Grith S.,Jeppesen, Lone,Mogensen, John P.,Pettersson, Ingrid,Jeppesen, Claus B.,Daugaard, Jens R.,Galsgaard, Elisabeth D.,Ynddal, Lars,Fleckner, Jan,Panajotova, Vladimira,Polivka, Zdenek,Pihera, Pavel,Havranek, Miroslav,Wulff, Erik M.
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p. 1495 - 1503
(2008/02/03)
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- COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
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Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. (Formula
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Page/Page column 40-41
(2008/06/13)
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- Calcilytic compounds
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Novel calcilytic compounds and methods of using them are provided.
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Page/Page column 6-7
(2010/02/05)
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- Regioselective synthesis of 1,8-dihydroxytetralins through a tandem reduction/intramolecular hydroxyalkylation of 4-(3-hydroxyphenyl)alkanoates
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A series of 4-(3-hydroxyphenyl)butanoates 3 has been prepared and transformed into 1,8-dihydroxytetralins of general formula 2 by treatment with 2 equivalents of DIBALH followed by quenching with aqueous NH4Cl. A possible mechanism for this novel totally regioselective intramolecular hydroxyalkylation is suggested and the factors affecting the stability of 1,8-dihydroxytetralins 2 are also discussed.
- Guanti, Giuseppe,Banfi, Luca,Riva, Renata
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p. 11945 - 11966
(2007/10/02)
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- Tandem Reduction / Intramolecular Hydroxyalkylation of (3-Hydroxyphenyl)alkanoates: a New Regioselective Approach to 1,8-Dihydroxytetralins
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4-(3-hydroxyphenyl)-butanoates 4, on treatment with DIBALH, followed by hydrolytic work-up, undergo a novel completely regioselective intramolecular hydroxyalkylation reaction to give 1,8-dihydroxytetralins.The yield of the reaction depends heavily on the structure of starting material, best results being achieved with 3,3-disubstituted butanoates.
- Guanti, Giuseppe,Banfi, Luca,Narisano, Enrica,Riva, Renata,Thea, Sergio
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p. 3919 - 3922
(2007/10/02)
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- SYNTHESIS AND CHEMISTRY OF AN IRON(III) TETRAPHENYLPORPHYRIN WITH A COVALENTLY-ATTACHED PHENOLATE TAIL
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We report the synthesis of a phenolate-tailed iron(III) tetraphenylporphyrin, 1.The phenolate ligand is covalently-attached to the porphyrin ring and is coordinated to the iron(III) center.This phenolate ligand increases the rate of oxygen atom transfer to the metal center.
- Nee, Michael W.,Kim, Chongwoo A.,Garg, Sandhya,Griffith, Michael C.,Mizoue, Laura S.,et al.
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p. 5345 - 5348
(2007/10/02)
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