The present invention provides a maleate, phosphate, sulfate, hydrochloride of a cyclohexane derivative, N′-[trans-4-[2-[7-(benzo[b]thiophene)-7-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea, as shown in Formula I and crystal forms thereof. The crystal forms have low hygroscopicity and good stability and are convenient for long-term storage and transportation; or the crystal forms have a long half-life in vivo, high bioavailability and small individual difference, and thus have obvious clinical application advantages.
C07D 333/66 - Nitrogen atoms not forming part of a nitro radical
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention provides a maleate, phosphate, sulfate, and hydrochloride of a cyclohexane derivative, N'-[trans-4-[2-[7-(benzo[b]thiophene)-7-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea, as shown in formula I and crystal forms thereof. The crystal forms have low hygroscopicity and good stability and are convenient for long-term storage and transportation; or the crystal forms have a long half-life in vivo, high bioavailability, and small individual differences, and thus have obvious clinical application advantages.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention provides a maleate, phosphate, sulfate, and hydrochloride of a cyclohexane derivative, N'-[trans-4-[2-[7-(benzo[b]thiophene)-7-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea, as shown in formula I and crystal forms thereof. The crystal forms have low hygroscopicity and good stability and are convenient for long-term storage and transportation; or the crystal forms have a long half-life in vivo, high bioavailability, and small individual differences, and thus have obvious clinical application advantages.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention provides a method for preparing a cyclohexane derivative, comprising the following steps: (1) subjecting a compound SM01 and a compound SM02 or a salt thereof to a nucleophilic substitution reaction to obtain a compound A; (2) deprotecting the compound A to obtain a compound B; and (3) subjecting the compound B and an acylation reagent to an acylation reaction to obtain a cyclohexane derivative. The method provided by the present invention has less side reactions, high product yield, and high product purity, and are suitable for industrial-scale production.
Provided is a method for preparing a cyclohexane derivative, the method comprising the following steps: subjecting a compound, 2-(4-(3,3-dimethylureido)cyclohexyl)acetaldehyde, represented by formula SM01 and a compound represented by formula SM02 to a condensation imine reduction reaction to obtain the cyclohexane derivative. The method of the present invention has few side reactions, a high product yield and a high product purity, and is favorable for the industrial scale production.
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 275/04 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
C07D 333/06 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
Disclosed are a new crystal form of a rosuvastatin calcium intermediate, [4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methanesulfonamido)-5-pyrimidyl]triphenylphosphonium bromide, and a preparation method therefor. The XRPD spectrum of the crystal form, which is measured by using CuKα irradiation and is represented by 2θ angles, has diffraction peaks at least at 7.475º ± 0.2º, 8.626º ± 0.2º, 9.414º ± 0.2º, 10.753º ± 0.2º, 11.382º ± 0.2º and 14.940º ± 0.2º. The crystal form has low hygroscopicity and good stability, and is convenient for long-term storage and transportation.
The present invention provides a genetically engineered bacterium of coexpressing cyclohexanone monooxygenase and isopropanol dehydrogenase and use thereof, and the genetically engineered bacterium constructed can catalyze and convert high-concentration omeprazole sulfide into esomeprazole.
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