摘要:
The invention relates to a process for preparing saturated or unsaturated lactones. This process involves reacting a bicyclic compound or a monocyclic compound with hydrogen peroxide in the presence of a first acid having a pK a of 3 or less and a first organic solvent, thereby forming a hydroperoxide. The obtained mixture comprising the hydroperoxide is subsequently metered to a mixture of a second organic solvent and a dissociation-enhancing catalyst, optionally comprising a second organic acid. The invention also pertains to a process of preparing the hydroperoxide.
摘要:
A process for cooxidizing organic compounds which comprises, in the presence of an imide compound such as N-hydroxyphthalimide, oxidizing with molecular oxygen a compound (A) which is selected from among (A1) compounds having nonaromatic ethylenic linkage and (A2) ketones or alcohols corresponding to the ketones and a compound (B) which can be oxidized by the above imide compound with oxygen and is different from the above compound (A). As the compound (B), use can be made of (a) primary or secondary alcohols (benzhydrol, cyclohexanol, etc.), and (b) compounds having a carbon-hydrogen bond adjacent to an unsaturated bond (tetralin, ethylbenzene, etc.). Use of this process makes it possible to obtain the corresponding epoxy compounds from (A1) compounds having nonaromatic ethylenic linkage, and the corresponding esters or lactones from (A2) ketones or alcohols corresponding to the ketones, each at a high yield.
摘要:
The present application describes modulators of MCP-1 of formula (I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and cancer.
摘要:
The invention relates to a method for hydrogenation of carbonyl compounds, in particular C4-dicarboxylic acids for producing mixtures of tetrahydrofuranne and gamma-butyrolactone on supported rhenium-containing catalysts. Said catalysts are characterised in that rhenium and at least another metal of groups VIII or Ib of the Periodic table of elements, in particular ruthenium (Ru), rhodium (Rh), palladium (Pd), osmium (Os), iridium (Ir), platinum (Pt), copper (Cu), silver (Ag) or cobalt (Co) in the form of at least one bimetallic precursor compound are applied to the support. The inventive catalysts are also disclosed.
摘要:
The invention relates to a method for hydrogenation of carbonyl compounds, in particular C4-dicarboxylic acids for producing mixtures of tetrahydrofuranne and gamma-butyrolactone on supported rhenium-containing catalysts. Said catalysts are characterised in that rhenium and at least another metal of groups VIII or Ib of the Periodic table of elements, in particular ruthenium (Ru), rhodium (Rh), palladium (Pd), osmium (Os), iridium (Ir), platinum (Pt), copper (Cu), silver (Ag) or cobalt (Co) in the form of at least one bimetallic precursor compound are applied to the support. The inventive catalysts are also disclosed.
摘要:
A process for preparing functionalized y-butyrolactones 3 and various biologically active compounds using mucohalic acid 1 and halide 2 in the presence of indium is disclosed, wherein X, Y, RI, R2, and R3 may have any of the meanings defined herein.
摘要:
Novel compounds of structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as, the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要:
A process for cooxidizing organic compounds which comprises, in the presence of an imide compound such as N-hydroxyphthalimide, oxidizing with molecular oxygen a compound (A) which is selected from among (A1) compounds having nonaromatic ethylenic linkage and (A2) ketones or alcohols corresponding to the ketones and a compound (B) which can be oxidized by the above imide compound with oxygen and is different from the above compound (A). As the compound (B), use can be made of (a) primary or secondary alcohols (benzhydrol, cyclohexanol, etc.), and (b) compounds having a carbon-hydrogen bond adjacent to an unsaturated bond (tetralin, ethylbenzene, etc.). Use of this process makes it possible to obtain the corresponding epoxy compounds from (A1) compounds having nonaromatic ethylenic linkage, and the corresponding esters or lactones from (A2) ketones or alcohols corresponding to the ketones, each at a high yield.
摘要:
A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site. Representative energy sources can be in the form of electric force, ultrasound. Light or radiation of a radioactive material which can be administered either externally or internally.