- Preparation method of 2 -bromo -4-chlorobenzaldehyde
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The invention relates to a preparation method of 2 -bromo -4-chlorobenzaldehyde and belongs to the field of medicinal chemistry. The preparation method can obtain 2 -bromo -4-chlorobenzaldehyde by taking nitrotoluene as a starting material through substitution, reduction, substitution, substitution, substitution, hydrolysis and elimination reaction. Compared with the prior art, the method shortens the reaction time, the reaction temperature is higher 120 °C or higher, the reaction conditions are mild, the yield of the obtained product is about 70% and more than 90%. The reaction temperature is reduced, high-boiling-point solvent is not needed to participate in the reaction, the post-treatment is simple, and the method is more suitable for industrial production with strict safety and environmental protection.
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Paragraph 0087-0089
(2021/08/25)
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- FACTOR XIa INHIBITORS
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The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
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Page/Page column 62
(2017/05/21)
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- Palladium-Catalyzed Ring-Forming Aminoalkenylation of Alkenes with Aldehydes Initiated by Intramolecular Aminopalladation
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A palladium-catalyzed aminopalladation reaction followed by nucleophilic addition with aldehydes and dehydration is described. This direct and operationally simple procedure provides a rapid and reliable approach to a wide range of functionalized tetrahydroisoquinolines with high selectivity. Mechanistic studies disclosed that the nucleophilic addition, performed via a highly ordered transition-state, is the turnover-limiting step in which the inherent β-hydride elimination of the key Csp3?Pd species was controlled by the confined conformation and the nucleophilicity of the Csp3?Pd bond was enhanced by the strong electron-donating effect of the nitrogen atom.
- Hu, Yue,Xie, Yinjun,Shen, Zhiqiang,Huang, Hanmin
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supporting information
p. 2473 - 2477
(2017/02/23)
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- FACTOR XIa INHIBITORS
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The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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Page/Page column 36
(2016/11/02)
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- NAPHTHYLACETIC ACIDS
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The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
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Page/Page column 72-73
(2010/06/15)
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- 6-SUBSTITUTED PHENOXYCHROMAN CARBOXYLIC ACID DERIVATIVES
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Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
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Page/Page column 63-64
(2010/01/30)
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- Synthesis and fungicidal activities of novel indene-substituted oxime ether strobilurins
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Nineteen novel indene-substituted oxime ether strobilurins, which used an indene group to stabilize the (E)-styryl group in SYP-Z071 (an unsaturated oxime strobilurin fungicide under development by the Shenyang Research Institute of Chemical Industry), were designed and synthesized. The biological assay results showed that all compounds possessed good or excellent fungicidal activities. It was found that most of the compounds showed higher fungicidal activities against Pyricularia oryzae, Phytophthora infestans, Erysiphe graminis, and Colletotrichum lagenarium than SYP-Z071 at the tested concentration. The biological assay results also indicated that most of the compounds exhibited higher in vivo fungicidal activities against cucumber Pseudoperonospora cubensis and C. lagenarium than the commercial fungicides trifloxystrobin and kresoxim-methyl at a concentration of 6.25 mg/L. Furthermore, it was found that α-(methoxyimino)-N-methylphenylacetamide oxime ethers 6m-s exhibited a broad spectrum and remarkably higher activities against all tested fungi. Especially, the 6-methylindene-substituted compound 6p was identified as the most promising candidate for further study.
- Tu, Song,Xu, Long-He,Ye, Li-Yi,Wang, Xi,Sha, Yong,Xiao, Zong-Yuan
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experimental part
p. 5247 - 5253
(2010/04/06)
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- Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors
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Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2,4-dichlorocinnamic acid hydroxamate, herein we report on the structure-activity relationship of a series of hydroxamate BoNT/A inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory activity to that of the lead structure.
- Capkova, Katerina,Yoneda, Yoshiyuki,Dickerson, Tobin J.,Janda, Kim D.
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p. 6463 - 6466
(2008/04/02)
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- 1-(HETERO)ARYL-3-AMINO-PYROLLIDINE DERIVATIVES FOR USE AS MGLUR3 RECEPTOR ANTAGONISTS
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The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.
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Page/Page column 47
(2010/11/08)
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