Patent classifications
C07D453/04
Three-Dimensional Organic Sandwich Chirality and Its Synthetic Assembly
The present invention includes a multi-layer 3D material, a method of making, and a catalyst comprising: a first, a second, and a third layer, wherein each of the layers are arranged in a nearly parallel fashion with chirality along a center plane.
Methods for extraction, processing, and purification of a selected family of target compounds from cannabis
Disclosed are methods for separating, recovering, and purifying tetrahydrocannabinolic acid (THCA) salts from an organic solvent solution comprising a mixture of cannabinoids. The methods comprise solubilizing the mixture of cannabinoids in a selected C5-C7 hydrocarbon solvent, adding thereto a selected amine to thereby precipitate a THCA-amine salt therefrom, dissolving the recovered THCA-amine salt in a selected solvent and then adding thereto a selected antisolvent to thereby recrystallize a purified THCA-amine salt therefrom. The recrystallized THCA-amine salt may be decarboxylated to form a mixture of Δ9-tetrahydrocannabinol (Δ9-THC) and amine. The Δ9-THC amine mixture may be acidified to separate the amine from Δ9-THC. The recovered Δ9-THC may be concentrated to produce a highly purified Δ9-THC. Also disclosed are THCA-amine salts produced with amines selected from groups of diamines, amino alcohols, and tertiary amines.
Methods for extraction, processing, and purification of a selected family of target compounds from cannabis
Disclosed are methods for separating, recovering, and purifying tetrahydrocannabinolic acid (THCA) salts from an organic solvent solution comprising a mixture of cannabinoids. The methods comprise solubilizing the mixture of cannabinoids in a selected C5-C7 hydrocarbon solvent, adding thereto a selected amine to thereby precipitate a THCA-amine salt therefrom, dissolving the recovered THCA-amine salt in a selected solvent and then adding thereto a selected antisolvent to thereby recrystallize a purified THCA-amine salt therefrom. The recrystallized THCA-amine salt may be decarboxylated to form a mixture of Δ9-tetrahydrocannabinol (Δ9-THC) and amine. The Δ9-THC amine mixture may be acidified to separate the amine from Δ9-THC. The recovered Δ9-THC may be concentrated to produce a highly purified Δ9-THC. Also disclosed are THCA-amine salts produced with amines selected from groups of diamines, amino alcohols, and tertiary amines.
Method for producing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4- chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclo-propylpropanoic acid and the crystalline form thereof for use as a pharmaceutical ingredient
The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.
Process for the preparation of isoxazoline compounds
This invention relates to processes for the preparation of antiparasitic isoxazoline compounds enriched in an enantiomer using quinine-based chiral phase transfer catalyst. The invention also relates to novel quinine-based phase transfer catalysts and to a toluene solvent form of the isoxazoline compound of the invention.
Process for the preparation of isoxazoline compounds
This invention relates to processes for the preparation of antiparasitic isoxazoline compounds enriched in an enantiomer using quinine-based chiral phase transfer catalyst. The invention also relates to novel quinine-based phase transfer catalysts and to a toluene solvent form of the isoxazoline compound of the invention.
FUNCTIONALIZED FLUOROALKYL SILANE, AND SYNTHETIC METHOD THEREFOR AND APPLICATION THEREOF
Disclosed in the present invention are a functionalized fluoroalkyl silane compound and a synthetic method therefor. The method comprises: dissolving a halosilane and a fluoroalkyl source in an organic solvent; and synthesizing functionalized fluoroalkyl silane under the effect of an alkali or a tertiary phosphine compound. The functionalized fluoroalkyl silane can not only be used for constructing a series of high added-value compounds such as fluoroalkyl substituted alcohols, ketones and amines that can be constructed by conventional TMSR.sub.f, but also can transfer, by means of appropriate conversion, a functional group on a silicon protecting group to the obtained addition product in an addition reaction, for synthesizing some fluorine-containing compounds that cannot be synthesized by using a conventional TMSR.sub.f reagent, thereby greatly improving the synthesis efficiency and the atom economy of reactions. Also disclosed in the present invention are more excellent reaction efficiency and enantioselectivity, compared with conventional TMSCF.sub.3, exhibited by trifluoromethyl chloromethylsilane in synthesis of a 2-trifluoromethylquinoline compound and in an asymmetric trifluoromethylation reaction with α,β-unsaturated ketones.
FUNCTIONALIZED FLUOROALKYL SILANE, AND SYNTHETIC METHOD THEREFOR AND APPLICATION THEREOF
Disclosed in the present invention are a functionalized fluoroalkyl silane compound and a synthetic method therefor. The method comprises: dissolving a halosilane and a fluoroalkyl source in an organic solvent; and synthesizing functionalized fluoroalkyl silane under the effect of an alkali or a tertiary phosphine compound. The functionalized fluoroalkyl silane can not only be used for constructing a series of high added-value compounds such as fluoroalkyl substituted alcohols, ketones and amines that can be constructed by conventional TMSR.sub.f, but also can transfer, by means of appropriate conversion, a functional group on a silicon protecting group to the obtained addition product in an addition reaction, for synthesizing some fluorine-containing compounds that cannot be synthesized by using a conventional TMSR.sub.f reagent, thereby greatly improving the synthesis efficiency and the atom economy of reactions. Also disclosed in the present invention are more excellent reaction efficiency and enantioselectivity, compared with conventional TMSCF.sub.3, exhibited by trifluoromethyl chloromethylsilane in synthesis of a 2-trifluoromethylquinoline compound and in an asymmetric trifluoromethylation reaction with α,β-unsaturated ketones.
Compositions and methods for the inhibition of pruritus
Pharmaceutical compositions comprising a molecular inhibitor of Npr1 are disclosed. Also disclosed are methods of treating, reducing, or preventing acute and/or chronic pruritus in a mammal comprising administering a pharmaceutical composition comprising a molecular inhibitor of Npr1.
Nitrosation Reagents and Methods
Provided are compounds that can find use as nitrosation reagents. Provided are nitrosation methods that include reacting a substrate with one of the provided nitrosation reagents and thereby generating a nitrosation product. Provided are kits including a nitrosation reagent. Provided are compositions wherein the nitrosation reagent is enriched in the .sup.15N isotope.