- Synthesis of 2 - fluoro aniline compounds of the method
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The invention discloses a method for synthesizing 2 - fluoro aniline compounds of the method, the method is: shown in formula Ia aniline compound of formula Ib α and β shown aniline compound as raw materials, through coupling reaction shown [...] azobenzene compound II, then the type II shown azobenzene compound with a palladium catalyst, fluorination reagent, additive, organic solvent, in the 30 - 150 °C temperature closed agitating the fluorination reaction, [...] compound of formula III, type III compounds are shown in the reaction under the action of a reducing [...] shown IV 2 - fluoro aniline compounds; this invention synthetic 2 - fluoro aniline compounds substrate wide adaptability, mild reaction conditions, the operation is simple, fluorinated and good selectivity, [...] aniline compounds is prepared by many drug molecule is an important intermediate and starting material, wide application prospects.
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- Anion ligand promoted selective C-F bond reductive elimination enables C(sp2)-H fluorination
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A detailed mechanism study on the anion ligand promoted selective C-H bond fluorination is reported. The role of the anion ligand has been clarified by experimental evidence and DFT calculations. Moreover, the nitrate promoted C-F bond reductive elimination enabled a selective C-H bond fluorination of various symmetric and asymmetric azobenzenes to access diverse o-fluoroanilines.
- Mao, Yang-Jie,Luo, Gen,Hao, Hong-Yan,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
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p. 14458 - 14461
(2019/12/09)
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- Compound and application of compound in preparation of medicines
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The invention discloses a compound and its application in a medicine. the invention specifically provides a compound as shown in the formula (I) or a stereisomer, a geometrical isomer, a tautomer, a racemate, nitric oxide, hydrate, a solvate, a metabolite, pharmaceutically acceptable salts or a prodrug of the compound as shown in the formula (I). The invention also discloses an application of the compound in preparation of a medicine. The medicine is used in treating cancers.
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Paragraph 0181; 0182; 0183
(2016/10/08)
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- NOVEL PYRIMIDINE DERIVATIVES 698
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The invention concerns compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.
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Page/Page column 174-175
(2008/12/07)
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- New spirocondensed quinazolinones and their use as phosphodiesterase inhibitors
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The invention relates to compounds of formula (I) wherein R1, R2 and m are as defined in the description, their use as medicament, pharmaceutical compositions containing them and a process for their preparation. These compounds act as Phosphodiesterase inhibitors and inhibit in particular PDE-7.
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- Novel compounds
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Compounds of general formula (I), R1 is selected from any one of phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl, and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; Ra and Rb is each and individually selected from any one of hydrogen, a straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
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- Substituted tricyclics
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A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA2mediated release of fatty acids for treatment of conditions such as septic shock.
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- Substituted carbazoles, process for their preparation and their use as sPLA2 inhibitors
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Novel tricyclics are disclosed together with the use of such compounds for inhibiting SPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
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- CHROMAN DERIVATIVES
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3-amino-5-carbamoylchromans and 8-fluoro-3-amino-5-carbamoylchromans, as well as enantiomers and salts thereof, are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.
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