CAS: 62613-82-5; 2-(4-Hydroxy-2-Oxopyrrolidin-1-yl)Acetamide

上下游产品

CAS号62613-81-4 4-羟基-2-氧代-1-吡咯烷乙酸乙酯 | CAS号10488-68-3 4-氯-3-羟基丁酸甲酯 | CAS号1668-10-6 甘氨酰胺盐酸盐 | CAS号4509-09-5 Methyl 3,4-epox... | CAS号154522-71-1 2-(4-hydroxypyr... | CAS号110104-61-5 ethyl (2,5-dihy... | CAS号113896-94-9 2-(5-oxo-3-phen... | CAS号85614-54-6 2,4-二氧代-1-吡咯烷乙酰胺

在 Palladium On Activated Charcoal Sodium Tetrahydroborate,甲烷磺酸,氨,氢气体系中,用 二甲胺 作为反应溶剂,15.0~55.0 °C,500.0 Kpa 条件下,反应 12.0H,反应生成 奥拉西坦
参考文献:用四酸中间体高效合成外消旋4-羟基-2-氧-1-吡咯烷乙酰胺(奥西西坦)
标题:用四酸中间体高效合成外消旋4-羟基-2-氧-1-吡咯烷乙酰胺(奥西西坦)
摘要:由(e)-4-氯-3-乙氧基丁-2-烯酸乙酯以消旋形式合成标题化合物1A,分五个步骤,总收率为43%.描述了最终产品的几种途径,但是最有效的途径涉及c(5)-未取代的四甲酸5B的氢化.这类化合物的不稳定性要求使用可以在非常酸性的水性条件下运行的催化剂,这种作用已被5%ru / C催化剂成功填补.
DOI:10.1002/hlca.19920750323

专利信息

专利号:US-10793521-B2
优先权日:2016-10-24
标 题:Crystalline form II of dextral oxiracetam, preparation method therefor and use thereof
发明人：YE LEI
权利人:CHONGQING RUNZE PHARMACEUTICAL; CHONGQING RUZER PHARMACEUTICAL COMPANY LTD
摘要:The present invention provides a crystalline form of dextral oxiracetam. The crystalline form has a diffraction peak when a diffraction angle, 2θ, is 17.76±0.2°, 20.16±0.2°, 21.20±0.2°, 24.17±0.2°, or 25.88±0.2°. The crystalline form of dextral oxiracetam can promote synthesis of phosphorylcholine and phosphoethanolamine, boosts cerebral metabolism, has a stimulating function on a specific central nervous pathway through a blood-brain barrier, and has special biological activity in the field of sedation and the antiepileptic field. The crystalline form of dextral oxiracetam of the present invention is a water-containing crystalline form, contains 0.5 water molecules, loses crystallization water at 73.5±2° C., and is melted and decomposed at 138.0±2° C. The crystalline form of dextral oxiracetam of the present invention can stably exist at room temperature and relative humidity of 0-95%, does not transform, is used for storage and formulation processing, and has low requirements for processing or storage humidity.

专利号:US-10696629-B2
优先权日:2016-10-24
标 题:Crystalline form of dextral oxiracetam, preparation method therefor and use thereof
发明人：YE LEI
权利人:CHONGQING RUNZE PHARMACEUTICAL
摘要:The present invention provides a crystalline form of dextral oxiracetam. The crystalline form has a diffraction peak when a diffraction angle, 2θ, is 17.12±0.2°, 18.88±0.2°, 19.24±0.2°, 21.18±0.2°, 24.88±0.2°. The crystalline form having oxiracetam can promote synthesis of phosphorylcholine and phosphoethanolamine, boosts cerebral metabolism, has a stimulating function on a specific central nervous pathway through a blood-brain barrier, improves the intelligence and memory, has an obvious effect on a memory dysfunction, and has special biologic activity in the field of sedation and the antiepileptic field. The method for preparing the crystalline form is simple and is suitable for industrial production.

专利号:US-10961192-B2
优先权日:2017-01-12
标 题:(R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, preparation method therefor, and application thereof
发明人：YE LEI
权利人:CHONGQING RUZER PHARMACEUTICAL COMPANY LTD
摘要:The present invention provides an (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, which has diffraction peaks when 2θ is 12.423±0.2°, 16.465±0.2°, 17.344±0.2°, 21.889±0.2°, and 25.054±0.2°. The present invention can promote synthesis of phosphorylcholine and phosphoethanolamine and promote cerebral metabolism, has a stimulating effect on the specific central nervous pathway through the blood-brain barrier, and has special biological activity in the fields of sedation, anti-epilepsy, etc. The (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form in the present invention has a melting point peak temperature of 133.1±2° C. and a solubility in water of greater than or equal to 100 mg/mL, dissolves fast in water, provides high bioavailability, good stability, and good particle fluidity, is suitable for production of pharmaceutical preparations and storage and transportation. The crystal form is suitable for preparation into a variety of pharmaceutical compositions, and can be prepared into a variety of preparations, such as tablets, capsules, dripping pills, sustained-release controlled-release preparations, lyophilized powder injections, etc. The preparation method of the present invention is simple and suitable for industrial production.

专利号:US-2009176740-A1
优先权日:2007-11-30
标题:Treatment of neurological conditions by the co-administration of aniracetam and l-alpha glycerylphosphorylcholine
发明人：PHILLIPS II DAUGLAS JAMES
权利人:PHILLIPS II DAUGLAS JAMES
摘要:Aniracetam (1-[(4-methoxybenzoyl)]-2-pyrrolidinone) is co-administered with the acetylcholine precursor 1-alpha glycerylphosphorylcholine (Alpha GPC, choline alfoscerate, choline alphoscerate) to potentiate cognition enhancing effects in healthy subjects and patients suffering from neurological conditions including Alzheimer's Disease (AD), attention deficit disorder (ADD), Parkinson's Disease, schizophrenia, vascular dementia, post stroke aphasia, anxiety disorders, cerebral atrophy, chronic alcoholism, Down syndrome, dyslexia, and various other neurodegenerative conditions. The co-administration of aniracetam (and other racetam derivatives including oxiracetam) with the acetylcholine precursor 1-alpha glycerylphosphorylcholine decreases negative side-effects such as severe headaches while increasing the synthesis and release of the neurotransmitters acetylcholine and glutamate to facilitate proper brain functioning.

专利号:WO-2018130062-A1
优先权日:2017-01-12
标题:Method for preparing (r)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form
发明人：YE LEI
权利人:CHONGQING RUZER PHARMACEUTICAL COMPANY LTD
摘要:The present invention provides a method for preparing an (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, which has diffraction peaks when 2θ is 12.423±0.2°, 16.465±0.2°, 17.344±0.2°, 21.889±0.2°, and 25.054±0.2°. The (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form prepared in the present invention can promote synthesis of phosphorylcholine and phosphoethanolamine and promote cerebral metabolism, has a stimulating effect on the specific central nervous pathway through the blood-brain barrier, and has special biological activity in the fields of sedation, anti-epilepsy, etc. The (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form prepared in the present invention has a melting point peak temperature of 133.1±2°C and a solubility in water of greater than or equal to 100 mg/mL, dissolves fast in water, provides high bioavailability, good stability, and good particle fluidity, and is suitable for production of pharmaceutical preparations and storage and transportation. The preparation method of the present invention is simple and suitable for industrial production.

专利号:CN-114180525-A
优先权日:2021-12-30
标题:A kind of separation method of hydrogen chloride/dichloromethane in the synthesis of ethyl 4-chloroacetoacetate