- A pharmaceutical intermediate 2 - methylamino -3 - pyridine methanol preparation method (by machine translation)
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The invention relates to a shakang [...] sulfate intermediate preparation method, the intermediate [...][...] sulfate for 2 - methylamino - 3 - pyridine methanol, comprising: make stated 2 - methylamino - 3 - pyridine carboxylic acid tert-butyl in the organic solvent and sodium borohydride or potassium borohydride/Lewis acid/Lewis acid in the presence of a reducing agent for the reduction of 2 - methylamino - 3 - pyridine methanol. The method of the invention low cost, high product yield and purity, mild condition, easy controlled, suitable for industrial production. (by machine translation)
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Paragraph 0021
(2019/10/22)
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- INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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The present invention provides a compound of formula (II): an inhibitor of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases. Its prodrugs are disclosed.
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- A preparation method of the midbody shakang zuo
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The invention relates to a preparation method of an isavuconazole intermediate. The isavuconazole intermediate is 2-methylamino-3-pyridylcarbinol. The method comprises the following steps: (1) reacting 2-chloronicotinic acid with methylamine dissolved in a methylamine solution to generate 2-methylamino-3-pyridylformic acid, wherein the methylamine solution is formed by dissolving methylamine in water, methanol or a water-methanol mixture; and (2) reducing the 2-methylamino-3-pyridylformic acid in a solvent in the presence of a reducer sodium borohydride/iodine, sodium borohydride/Lewis acid or red aluminum to obtain the 2-methylamino-3-pyridylcarbinol. The method has the advantages of low cost, high product yield and purity, and mild and controllable conditions, and is suitable for industrial scale-up production.
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Paragraph 0039-0046
(2018/05/16)
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- RING-FUSED 2-PYRIDONE DERIVATIVES AND HERBICIDES
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Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C═O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.
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Page/Page column 69
(2011/12/12)
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- N-substituted carbamoyloxyalkyl-azolium derivatives
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N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.
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Page/Page column 21-24; 36
(2010/02/09)
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- Design, synthesis and antifungal activity of a novel water soluble prodrug of antifungal triazole.
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A highly potent water soluble triazole antifungal prodrug, RO0098557 (1), has been identified from its parent, the novel antifungal agent RO0094815 (2). The prodrug includes a triazolium salt linked to an aminocarboxyl moiety, which undergoes enzymatic activation followed by spontaneous chemical degradation to release 2. Prodrug 1 showed high chemical stability and water solubility and exhibited strong antifungal activity against systemic candidiasis and aspergillosis as well as pulmonary aspergillosis in rats.
- Ohwada, Jun,Tsukazaki, Masao,Hayase, Tadakatsu,Oikawa, Nobuhiro,Isshiki, Yoshiaki,Fukuda, Hiroshi,Mizuguchi, Eisaku,Sakaitani, Masahiro,Shiratori, Yasuhiko,Yamazaki, Toshikazu,Ichihara, Shigeyasu,Umeda, Isao,Shimma, Nobuo
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p. 191 - 196
(2007/10/03)
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- Substituted 1,3-Dihydro-2H-pyrrolopyridin-2-ones as Potential Antiinflammatory Agents
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A series of analogues based on the 1,3-dihydro-2H-pyrrolopyridin-2-one ring system have been synthesized and shown to possess oral antiinflammatory activity in both the reverse passive Arthus reaction (RPAR) pleural cavity assay in rats and in the adjuvant-induced arthritic rat model (AAR).Several members of this series additionally exhibit an inhibitory effect on the in vivo production of prostaglandin- and leukotriene-derived products or arachidonic acid metabolism although these compounds exhibit no significant inhibitory activity against the cyclooxygenase and 5-lipoxygenase enzymes in vitro.Structure-activity relationships in this series are discussed.
- Ting, Pauline C.,Kaminski, James J.,Sherlock, Margaret H.,Tom, Wing C.,Lee, Joe F.,et al.
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p. 2697 - 2706
(2007/10/02)
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