摘要:
The present invention relates to a novel improved process and intermediates for the process of preparing the oxime intermediates of formula (II) wherein R1 is hydrogen, fluoro or chloro, and R2 is methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, cyano, fluoro, chloro or bromo. The novel process comprises diazotizing an aniline of formula (VI) reacting the resulting diazonium salt with isopropenylacetate of formula (X) and reacting the resulting ketone of formula (XI) with an organic nitrite in the presence of hydrogene chloride, and methylating the resulting ketooxime of formula (VIII) with a methylating agent and reacting the resulting O-methyl ketooxime of formula (IX) with hydroxylamine. The compounds of formula (II) are intermediates for highly active fungicides from the class of the strobilurins.
摘要:
Disclosed herein are methods for obtaining aza-pyridone compounds, which can be useful for ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection.
摘要:
Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要:
Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
摘要:
Disclosed are compounds and compositions that inhibit the action of monoacylglycerol lipase (MGL) and fatty acid amide hydrolase (FAAH), methods of inhibiting MGL and FAAH, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors.
摘要:
The catalytic hydrogenation of α,β-unsaturated ketones R 1 -CH=CH-CO-R 2 in which R 1 and R 2 independently of one another represent straight-chain or branched C 1 -C 12 -alkyl or C 2 -C 12 -hydroxyalkyl, straight-chain or branched C 2 -C 12 -alkenyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkenyl, C 7 -C 14 -aralkyl or C 6 -C 12 -aryl, where at least one of R 1 and R 2 is monosubstituted to trisubstituted by halogen, to give the respective saturated ketones R 11 -CH2-CH2-CO-R 12 in which R 11 and R 12 assume the meaning of R 1 and R 2 with the exception that alkenyl and cycloalkenyl are hydrogenated to the respective alkyl or cycloalkyl, wherein the hydrogenation process comprises combining the α,β-υnsaturated ketones and a reaction medium comprising a C 4 -C 10 alcohol and water in about a 1:2 to about a 2:1 mass ratio, and the hydrogenation is earned out in the presence of (i) basic substance comprising organic amine, (ii) Ni-containing catalyst, and (iii) organic sulphur compound.
摘要:
Die vorliegende Erfindung betrifft substituierte Cyclopenten-Derivate, ein Verfahren zu ihrer Herstellung sowie ihre Verwendung zur Herstellung von Arzneimitteln, insbesondere zur Behandlung und/oder Prävention von thromboembolischen Erkrankungen.
摘要:
The invention provides methods for treating beta-Amyloid protein-induced disease, pharmaceutical compositions and compounds useful for the same, and the use of these compounds for the manufacture of a medicament for treating the same. More particularly, the invention relates to the use of natural product compounds isolated from turmeric, gingko biloba, and ginger, and synthetic chemical analogues thereof, for the treatment of a beta-Amyloid protein-induced disease.
摘要:
1-(4-chlorophenyl)-4,4-dimethyl-pentane-3-one of formula (I) is prepared by the alkylation of pinacolone (3,3-dimethyl-2-butanone) with p-chlorobenzylchloride where the pinacolone is used both as a reagent and the solvent. The alkylation is done under either Phase Transfer Catalysis conditions in the presence of a base or in the presence of a strong base.