CAS: 928659-70-5; N-((1R,2R)-1-(2,3-Dihydrobenzo[b][1,4]Dioxin-6-yl)-1-Hydroxy-3-(Pyrrolidin-1-yl)Propan-2-yl)Octanamide ((2R,3R)-2,3-Dihydroxysuccinate)(2:1)
该化合物是一种合成化合物,主要用作治疗高氏病的药剂,高氏病是一种遗传性疾病,因酶胆碱酯酶缺乏而导致的遗传障碍.它作为一种减少基质疗法发挥作用,抑制了甘基二酰丙酰胺合成,从而减少了细胞中的累积.该物质的特征是其分子配方,反映了其复杂结构,而且通常看起来像一种白色到白色的粉末.埃利格鲁斯特酸盐在标准储存条件下是水溶的,并且具有稳定性.其行动机制包括选择性抑制甘基酰环己氨基合成酶酶,这对于其治疗效果至关重要.该化合物是口服的,具有有利的致癌性剖析特征,允许一次性服用.与任何药物一样,潜在的副作用可能包括胃肠扰动和其他系统反应,因此在治疗期间必须进行监测.
- 英文名称N-((1R,2R)-1-(2,3-Dihydrobenzo[b][1,4]Dioxin-6-yl)-1-Hydroxy-3-(Pyrrolidin-1-yl)Propan-2-yl)Octanamide ((2R,3R)-2,3-Dihydroxysuccinate)(2:1)
- 中文名称依利格鲁司特酒石酸盐
- IUPAC名称N-((1R,2R)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)octanamide ((2R,3R)-2,3-dihydroxysuccinate)(2:1)
- CAS编号928659-70-5
- MFCD编号:MFCD22665712
- FDA UNII编号:N0493335P3
- 分子式:C50H78N4O14分子量:959.19
- 产品CID: 1967356
- 同类组份化合物CAS491833-29-5 (free base)928659-70-5 (tartrate)
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
- 相似结构搜索
- InChIKey: KUBARPMUNHKBIQ-VTHUDJRQSA-N
- KUBARPMUNHKBIQ-VTHUDJRQSA-N
- 计算化学: 氢键受体数11.0氢键供体数6.0可旋转键数14.0
物理性质
合成工艺路线路线简述
📜在 Sodium Azide,草酰氯,Lithium Hydroxide Monohydrate,Palladium 10% On Activated Carbon,水,氢气,三乙胺,N,N-二甲基甲酰胺,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,二氯甲烷,水,N,N-二甲基甲酰胺 作为反应溶剂,20.0 °C,121.6 Kpa 条件下,反应 12.5H,反应生成 依利格鲁司特酒石酸盐
参考文献:一种高纯度依利格鲁司他的制备方法
标题:一种高纯度依利格鲁司他的制备方法
摘要:本发明涉及一种戈谢氏病治疗药物依利格鲁司他的制备方法,以s‑异丙基‑2‑噁唑烷酮为原料,经缩合反应,溴代反应,取代反应,水解反应,缩合反应以及还原反应得到依利格鲁司他;依利格鲁司他再经成盐和两部纯化步骤,得到高纯度的酒石酸依利格鲁司他.本发明从起始物料开始,对手性中心进行全合成,在减少反应步骤,缩短生产周期的同时,提高了手性中心的合成效率,并提高终产物收率,成盐步骤详细优化,保证了原料药的合格质控.
专利信息
专利号:US-9988364-B1
优先权日:2017-03-21
标题 :Process for synthesis of Eliglustat and intermediate compounds thereof
发明人：LIU YU; YU GUANNENG; ZHENG ZHIGUO
权利人:ZHEJIANG AUSUN PHARMACEUTICAL CO LTD
摘要:The present invention relates to a process for synthesis of Eliglustat and intermediate compounds thereof. In particular, the present invention relates to a process for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and relates to the intermediate compounds in the process and a process for preparation of the intermediate compounds.
专利号:US-10077458-B2
优先权日:2014-02-17
标题 :Microbiological process
发明人：ALVAREZ-RUIZ EMILIO; COLLIS ANDREW JOHN; DANN ALISON SARAH; FOSBERRY ANDREW PETER; READY SARAH JANE; VAZQUEZ MUNIZ MARIA JESUS
权利人:GLAXOSMITHKLINE IP DEV LTD
摘要:A process for the microbial synthesis of migalastat, specifically a process for the production of migalastat comprising culturing a microorganism under conditions such that at least one imino sugar is produced and detecting and/or isolating an imino sugar produced by said microorganism, and the microorganisms used in this process. The invention also comprises migalastat produced according to the above method and pharmaceutical compositions and uses thereof.
专利号:AU-2020409711-A1
优先权日:2019-12-20
标题 :Synthesis of lactone derivatives and their use in the modification of proteins
专利号:EP-4076533-A1
优先权日:2019-12-20
标 题:Synthesis of lactone derivatives and their use in the modification of proteins
专利号:CA-3164962-A1
优先权日:2019-12-20
标题 :Synthesis of lactone derivatives and their use in the modification of proteins
专利号:US-11697644-B2
优先权日:2017-03-21
标 题:Process for synthesis of eliglustat and intermediate compounds thereof
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Murugesan V, Chuang WL, Liu J, Lischuk A, Kacena K, Lin H, Pastores GM, Yang R, Keutzer J, Zhang K, Mistry PK. Glucosylsphingosine is a key biomarker of Gaucher disease. Am J Hematol. 2016 Nov;91(11):1082-1089. doi: 10.1002/ajh.24491.
3: Belmatoug N, Di Rocco M, Fraga C, Giraldo P, Hughes D, Lukina E, Maison-Blanche P, Merkel M, Niederau C, Plӧckinger U, Richter J, Stulnig TM, Vom Dahl S, Cox TM. Management and monitoring recommendations for the use of eliglustat in adults with type 1 Gaucher disease in Europe. Eur J Intern Med. 2016 Aug 10. pii: S0953-6205(16)30217-5. doi: 10.1016/j.ejim.2016.07.011. [Epub ahead of print] Review. doi: 10.2147/TCRM.S108027.
6: Ibrahim J, Underhill LH, Taylor JS, Angell J, Peterschmitt MJ. Clinical response to eliglustat in treatment-naïve patients with Gaucher disease type
合成参考文献
参考文献:10.1007/978-3-662-63709-8_90
摘要:Rupec RA. Disorders of Purine, Sphingolipid, and Amino Acid Metabolism. 2022. In: Braun-Falco´s Dermatology.
参考文献:10.1186/s43042-024-00552-z
摘要:El-Beshlawy A, Tantawy AAG, Shawky RM, Elsayed SM, Marzouk IM, Elgawhary S, Abdelghaffar H, Safy UE, Eid K, EISayh KI, Megahed A, Adly A, Sherif EM, Youssef MAM, Fathy MM, Salah NY, Elzeiny SM, EI Bakky ERAA, Fateen E. Diagnosis and management of patients with Gaucher disease: an Egyptian expert opinion. Egypt J Med Hum Genet. 2024 Jul 31;25(1). doi: 10.1186/s43042-024-00552-z.
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