5-(3-二甲氨基丙基)-10,11-二氢二苯并[a,D]环庚烯-5-醇 以 乙醇 作为反应溶剂,200.0 °C,11.0 Mpa 条件下,反应 0.01H,以78%的收率获得产物阿米替林 参考文献:阿米替林连续流合成中的多种有机锂反应生成 标题:阿米替林连续流合成中的多种有机锂反应生成 摘要:Abstracta Continuous Flow Protocol For The Preparation Of The Tricyclic Antidepressant (Tca) Amitriptyline Is Reported. The Advantages Of Flow Chemistry When Handling Organometallic Agents As Well As When Performing Reaction With Gases Are Demonstrated. Continuous Multilithiation Combined With Carboxylation And The Parham Cyclization,A Grignard Addition And Thermolytic Water Elimination By Inductive Heating Are Key Features Of The Multistep Protocol.Magnified Image DOI:10.1002/adsc.201300614
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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-12234200-B2 优先权日:2019-04-16 标 题:Synthetic methods of preparing esketamine 发明人:CHEN CHENG YI 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.
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-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
1: Han FY, Kuo A, Nicholson JR, Corradinni L, Smith MT. Comparative Analgesic Efficacy of Pregabalin Administered According to Either a Prevention Protocol or an Intervention Protocol in Rats with Cisplatin-induced Peripheral Neuropathy. Clin Exp Pharmacol Physiol. 2018 May 21. doi: 10.1111/1440-1681.12971. [Epub ahead of print] doi: 10.1002/14651858.CD010753.pub2. [Epub ahead of print] Review. doi: 10.1016/j.talanta.2018.03.103. Epub 2018 Apr 3. doi: 10.1016/j.talanta.2018.03.102. Epub 2018 Apr 3. doi: 10.1097/PR9.0000000000000638. eCollection 2018 Mar. 7: Bruno MAD, Krymchantowski AV. Amitriptyline and intraoral devices for migraine prevention: a randomized comparative trial. Arq Neuropsiquiatr. 2018 Apr;76(4):213-218. doi: 10.1590/0004-282x20180023. pii: 18f12254. doi: 10.4088/JCP.18f12254. doi: 10.1016/j.biocel.2018.04.017. [Epub ahead of print] doi: 10.1016/j.jad.2018.04.080. Epub 2018 Apr 16. doi: 10.11607/ofph.2023. doi: 10.1002/14651858.CD008581.pub2. Review. doi: 10.1016/j.envpol.2018.04.039. Epub 2018 Apr 19. doi: 10.1016/j.jhazmat.2018.03.050. [Epub ahead of print] doi: 10.1016/j.scitotenv.2018.03.278. Epub 2018 Apr 5.
合成参考文献
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:10.1177/1049909111412539 摘要:Mishra S, Bhatnagar S, Goyal GN, Rana SP, Upadhya SP. A comparative efficacy of amitriptyline, gabapentin, and pregabalin in neuropathic cancer pain: a prospective randomized double-blind placebo-controlled study. Am J Hosp Palliat Care. 2012 May;29(3):177–82. doi: 10.1177/1049909111412539. 参考文献:10.1155/2011/903595 摘要:Ooi C, Zawar V. Hyperaesthesia Following Genital Herpes: A Case Report. Dermatology Research and Practice. 2011;2011():1–3. doi: 10.1155/2011/903595. 参考文献:10.1007/s12028-011-9580-1 摘要:Schirmer CM, Kornbluth J, Heilman CB, Bhardwaj A. Gastrointestinal prophylaxis in neurocritical care. Neurocrit Care. 2012 Feb;16(1):184–93. doi: 10.1007/s12028-011-9580-1.