CAS: 123441-03-2; (S)-3-(1-(Dimethylamino)Ethyl)Phenyl Ethyl(Methyl)Carbamate

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17H18N2O5C17H18N2O5 N-Ethylmethylamine N-ethyl-N-methylcarbamoyl chloride rivastigmine hydr°Chloride(S)-3-(1-dimethylaminoethyl)phenol N-Ethylmethylamine carbon dioxide 3-(1-methoxyethyl)phenyl N-ethyl-N-methylcarbamate

合成工艺路线路线简述

  • 合成目标产物 Rivastigmine 主要起始原料 Ethylmethyl-Carbamic Chloride
  • (文献来源)合成步骤主要原料 Ethylmethyl-Carbamic Chloride
Rivastigmine Hydrochloride置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 0.5H,以66.3%的收率获得利凡斯的明
参考文献:Wo2006/68386
标题:Wo2006/68386

海关参考信息

专利信息


专利号:US-2003083352-A1
优先权日:2000-07-31
标 题 :Synthesis of imidazole intermediates
发明人:HELAL CHRISTOPHER J
权利人:PFIZER
摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.

专利号:WO-2018158674-A1
优先权日:2017-03-03
标 题 :Asymmetric synthesis of (s)-3-(1-(dimethylamino) ethyl) phenylethyl(methyl)carbamate and its salts
发明人:SAHAY RAKESH; ROY ANJAN
权利人:TROY LIFE SCIENCES
摘要:The present invention is in relation to a process of preparation of asymmetric synthesis of Rivastigmine and its salts in high yield and purity.

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-2024082118-A1
优先权日:2021-05-19
标 题:Topical compositions and methods of preparing the same
发明人:ABRAMOVICH SAGI; AVIDOR GAL; LANDA BENZION
权利人:LANDA LABS 2012 LTD
摘要:There is disclosed a composition comprising a water-insoluble thermoplastic compound capable of stimulating collagen synthesis (CSSC), the CSSC having a molecular weight of more than 0.6 kDa and being dispersed in a polar carrier as nano-elements having an average diameter of 200 nm or less and a viscosity of 107 mPa·s or less. The nano-elements of CSSC can be capable of stimulating the synthesis of skin proteins and/or enabling the delivery of active agents upon their application to a surface to be treated therewith. Methods for preparing the compositions and uses thereof are also provided.

专利号:US-8067465-B2
优先权日:2002-01-15
标题:Tricyclic-bis-enone derivatives and methods of use thereof
发明人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO
权利人:HONDA TADASHI; FAVALORO FRANK G; GRIBBLE GORDON W; SPORN MICHAEL B; SUH NANJOO; DARTMOUTH COLLEGE
摘要:Novel tricyclic-bis-enone derivatives (TBEs) as well as the process for the preparation of such TBEs are provided. Also provided are methods for prevention and/or treatment of cancer, Alzheimer's disease, Parkinson's disease, multiple sclerosis, amyotropic lateral sclerosis, rheumatoid arthritis, inflammatory bowel disease, and all other diseases whose pathogenesis is believed to involve excessive production of either nitric oxide (NO) or prostaglandins or the overexpression of iNOS or COX-2 genes or gene products. Further, methods for the synthesis of the TBE compounds of the invention utilize cheap commercially available reagents and are highly cost effective and amenable to scale-up. Additional high efficiency synthetic methods that utilize novel intermediates as well as the synthesis of these intermediates are also provided. Furthermore, the invention also provides methods for designing novel and water-soluble TBEs.

专利号:US-2002040032-A1
优先权日:2000-07-07
标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system
发明人:GLASKY MICHELLE S; LAHIRI DEBOMOY K; FARLOW MARTIN R
摘要:A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.
东晟凯瑞(上海)医药科技有限公司
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主要参考文献


1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Rivastigmine. 2020 Jan 15. 3(2):211-25.
3: Siddiqui MA, Wagstaff AJ. Rivastigmine: in Parkinson's disease dementia. CNS Drugs. 2006;20(9):739-47; discussion 748-50. doi: 10.2165/00023210-200620090-00003. 9(5):230-4. doi: 10.1097/01.nrl.0000087724.73783.5f. 38(2):15-6. 13(5):391-411. doi: 10.2165/00002512-199813050-00005.
12:697-707. doi: 10.2147/CIA.S129145.

合成参考文献


参考文献:10.1007/bf03327445
摘要:Panza F, Solfrizzi V, Frisardi V, Imbimbo BP, Capurso C, D’Introno A, Colacicco AM, Seripa D, Vendemiale G, Capurso A, Pilotto A. Beyond the neurotransmitter-focused approach in treating Alzheimer’s Disease: drugs targeting β-amyloid and tau protein. Aging Clinical and Experimental Research. 2009 Dec;21(6):386–406. doi: 10.1007/bf03327445.
参考文献:10.1016/j.neuropharm.2010.02.010
摘要:Francis PT, Ramírez MJ, Lai MK. Neurochemical basis for symptomatic treatment of Alzheimer's disease. Neuropharmacology. 2010 Sep;59(4-5):221–9. doi: 10.1016/j.neuropharm.2010.02.010.
参考文献:10.1186/1471-2377-10-14
摘要:Liu-Ambrose T, Eng JJ, Boyd LA, Jacova C, Davis JC, Bryan S, Lee P, Brasher P, Hsiung GY. Promotion of the mind through exercise (PROMoTE): a proof-of-concept randomized controlled trial of aerobic exercise training in older adults with vascular cognitive impairment. BMC Neurol. 2010 Feb 17;10():14.
参考文献:10.3390/ijms12063648
摘要:Ashraf MW, Tayyaba S, Afzulpurkar N. Micro Electromechanical Systems (MEMS) Based Microfluidic Devices for Biomedical Applications. Int J Mol Sci. 2011;12(6):3648–704.
参考文献:10.1111/j.1532-5415.2011.03468.x
摘要:Naharci IM, Bozoglu E, Karadurmus N, Karaman M, Kurt O, Doruk H. Rivastigmine associated hyponatremia in an older patient with Alzheimer's disease. J Am Geriatr Soc. 2011 Jul;59(7):1351–2. doi: 10.1111/j.1532-5415.2011.03468.x.
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