- Continuous synthesis method for substituted benzoic acid organic matter
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The invention provides a continuous synthesis method for a substituted benzoic acid organic matter. The continuous synthesis method comprises the following steps: in the presence of a catalyst and anorganic solvent, continuously putting an organic matter of a formula (I) shown in the specification, and oxygen into a continuous reaction device, carrying out a continuous oxidation reaction so as toobtain the substituted benzoic acid organic matter, and continuously discharging the substituted benzoic acid organic matter, wherein the substituted benzoic acid organic matter is of a structure ofa formula (II) shown in the specification. Oxygen is a green reagent and is cheap and easy to obtain, a great amount of wastes are not generated after reactions are completed, and the system is easy to treat. Due to continuous reaction operation, the risk that the solvent has flash evaporation explosion because of high-concentration oxygen in in-batch reactions can be reduced. Under same oxidationconditions, due to a continuous preparation process, escape of oxygen can be reduced, the utilization rate of oxygen can be greatly increased, operation can be also simplified, the security of reactions can be improved, and the yield of the substituted benzoic acid organic matter can be increased.
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Paragraph 0132-0134; 0138
(2019/10/01)
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- TRIAZOLONE COMPOUNDS AS mPGES-1 INHIBITORS
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The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 110
(2014/01/08)
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- 2-Amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors
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The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.
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Page/Page column 15-16
(2012/12/13)
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- 2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS
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The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.
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Page/Page column 31
(2012/12/13)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- Compounds having activity as inhibitors of cytochrome P450RAI
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Compounds having Formula 1 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
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Page column 53
(2010/01/31)
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- Compounds having activity as inhibitors of cytochrome P450RAI
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Compounds having Formula 2 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
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Page column 51
(2010/01/31)
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- Compounds having activity as inhibitors of cytochrome P450RAI
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Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
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Page column 26,51
(2010/11/29)
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- The basicity gradient-driven migration of iodine: Conferring regioflexibility on the substitution of fluoroarenes
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Six different fluoroarenes were submitted to the same transformations. Direct deprotonation with alkyllithium or lithium dialkylamide as reagents and subsequent carboxylation afforded the acids 1, 6, 11, 16, 18, and 23. If the aryllithium intermediate was trapped with iodine rather than with dry ice, an iodofluoroarene (2, 7, 12, 17, 19, and 24) was formed. This, upon treatment with lithium diisopropylamide, underwent deprotonation and iodine migration. The resulting new aryllithium species was intercepted either by carboxylation, to give the acids 3, 8, 13, 20, and 25, or by neutralization, to produce the iodofluoroarenes 4, 9, 14, 21, and 26. The latter family of compounds was converted into another set of acids 5, 10, 15, 22, and 27 by subsequent treatment with butyllithium or isopropylmagnesium chloride and carbon dioxide. ( Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002).
- Rausis, Thierry,Schlosser, Manfred
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p. 3351 - 3358
(2007/10/03)
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- Trisubstituted phenyl derivatives having retinoid agonist, antagonist or inverse agonist type biological activity
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Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.
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- Substituted diaryl or diheteroaryl methanes, ethers and amines having retinoid agonist, antagonist or inverse agonist type biological activity
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Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.
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- Liquid crystal compounds and optically active compounds
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A compound usefull for liquid crystal component which is represented by the following formulas (1), (2), (3), or (4) ;, R1 -X1 -A1 -( A2 )n-Y1 -A3 -X2 -R2 (1), R1 -X1 -( A3 -Y1 )N-A1 -A2 -X2 -R2 (2), R3 -X1 -A4 -Y1 -A3 -X2 -R4 (3), R3 -X1 -A5 -Y1 -A1 -A2 -X2 -R4 (4), wherein R1 ,R2 ,R3 and R4 are C1 18 alkyl groups; X1 and X2 is -, O, S, -C≡C- or divarent groups such as COO, OCO, CH2 O or OCH2
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- Pyrido[2,3-d]pyrimidine derivatives
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Derivatives of N-[2-(5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-6-yl)-alkyl]benzoyl-L-glutamic acid are antineoplastic agents. A typical embodiment is N-(2-fluoro-4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-gluta
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