合成目标产物 Tetracaine 主要起始原料 1-Bromobutane And Dimethylprocaine
38152-18-0 = 94-24-6 反应条件:1.1 Reagents: Dabco Catalysts: Dibromo[1,2-Di(Methoxy-Ko)Ethane]Nickel,2,4,5,6-Tetra(9H-Carbazol-9-Yl)Isophthalonitrile Solvents: Dimethylacetamide; 2 H,60 °C 标题:General Cross-Coupling Reactions With Adaptive Dynamic Homogeneous Catalysis 作者:Ghosh,Indrajit; Shlapakov,Nikita; Karl,Tobias A.; Dueker,Jonas; Nikitin,Maksim; Et Al 参考文献:Nature (London 日期:2023 卷标:619(7968) 页码:87-93]
71839-12-8 = 94-24-6 反应条件:1.1 Reagents: Sodium Methoxide; 8 H,130 °C 标题:Chemoselective Synthesis Of Tertiary And Secondary Amines By Reductive Amination Of Aldehydes 作者:Xiong,Wan-Jin; Li,Lei; Li,Jiang-Tao; Zhang,Shi-Qiang; Tang,Jun-Lei; Et Al 参考文献:Tetrahedron Letters 日期:2023 卷标:127]
38152-18-0 = 94-24-6 反应条件:1.1 Reagents: Dabco Catalysts: Dibromo[1,2-Di(Methoxy-Ko)Ethane]Nickel,Tris(2,2′-Bipyridine)Ruthenium(2+) Bis(Hexafluorophosphate) Solvents: Dimethyl Sulfoxide; 80 °C 标题:Visible Light-Mediated (Hetero)Aryl Amination Using Ni(Ii) Salts And Photoredox Catalysis In Flow: A Synthesis Of Tetracaine 作者:Park,Boyoung Y.; Pirnot,Michael T.; Buchwald,Stephen L. 参考文献:Journal Of Organic Chemistry 日期:2020 卷标:85(5) 页码:3234-3244]
4740-24-3 = 94-24-6 反应条件:1.1 Reagents: Sulfuric Acid Solvents: Toluene 标题:A Process For Preparing Tetracaine 参考文献:China]
2770284-53-0 = 94-24-6 反应条件:1.1 Reagents: Diphenylsilane Catalysts: Phosphetane,1,2,2,4-Tetramethyl-,1-Oxide Solvents: Cyclopentyl Methyl Ether; 48 H,120 °C 标题:Enabling Reductive C-N Cross-Coupling Of Nitroalkanes And Boronic Acids By Steric Design Of P(Iii)/p(V)=o Catalysts 作者:Li,Gen; Kanda,Yuzuru; Hong,Seung Youn; Radosevich,Alexander T. 参考文献:Journal Of The American Chemical Society 日期:2022 卷标:144(18) 页码:8242-8248]
= 94-24-6 [标题:Reaction Conditions 标题:Effect Of Noxyflex (Noxythiolin) On The Behavior Of Animals Which Have Been Infected Intraperitoneally With Suspensions Of Faeces 作者:Haler,David 参考文献:Internationale Zeitschrift Fuer Klinische Pharmakologie 日期:1974 卷标:9(2) 页码:160-4]
94-32-6 = 94-24-6 反应条件:1.1 Reagents: Sodium Methoxide; Rt -> 135 °C; 16 H,135 °C 标题:Cobalt Catalyzed Chemoselective Reduction Of Nitroarenes: Hydrosilylation Under Thermal And Photochemical Reaction Conditions 作者:Panda,Surajit; Nanda,Amareshwar; Behera,Rakesh R.; Ghosh,Rahul; Bagh,Bidraha 参考文献:Chemical Communications (Cambridge 日期:2023 卷标:59(30) 页码:4527-4530]
94-32-6 = 94-24-6 反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Ethanol,Toluene; Rt -> 120 °C; 3 H,120 °C 标题:Preparation Method Of Tetracaine,And Its Application In Preparation Of Tetracaine Hydrochloride 参考文献:China]
4740-24-3 = 94-24-6 反应条件:1.1 Reagents: Sulfuric Acid Solvents: Xylene; Reflux 标题:Method For Preparation Of Tetracaine Hydrochloride 参考文献:China]
= 94-24-6 [标题:Reaction Conditions 标题:Process For Purification Of 4-(Butylamino)-Benzoic Acid 2-(Dimethylamino)Ethyl Ester Hydrochloride 参考文献:China]
= 94-24-6 [标题:Reaction Conditions 标题:Co-Crystals Of Calixarenes And Biologically Active Molecules 参考文献:France]
= 94-24-6 [标题:Reaction Conditions 标题:The Effect Of Verapamil,Lanthanum And Local Anesthetics On Serotonin Release From Rabbit Platelets 作者:Zilberman,Yael; Gutman,Yehuda; Koren,Ruth 参考文献:Biochimica Et Biophysica Acta 日期:1982 卷标:691(1) 页码:106-14
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-2017165371-A1 优先权日:2017-02-22 标 题:Novel synthesis of potential ester prodrugs 发明人:GOLDBERG JOEL STEVEN 权利人:GOLDBERG JOEL STEVEN 摘要:Esters prodrugs that cross the blood brain barrier can be ideal drugs for treatment of diseases of the central nervous system because the cerebral spinal fluid contains an abundance of esterases. The prodrug can be hydrolyzed into an active drug and a metabolite such as cholesterol that is known to be non-toxic and is familiar to the central nervous system. This invention describes a modification of the Fischer-Speier or Fischer esterification reaction in which one reagent is lipophilic and the other reagent is hydrophilic. The reaction occurs in a heterogeneous mixture. The preferred catalyst is 1.0 M hydrochloric acid and the preferred solvent is acetone. The presence of ester synthesis was confirmed by the hydroxamic acid-ferric perchlorate reaction. The synthesis can be conducted without chemical scaffolds and without protecting functional groups.
专利号:US-2003050305-A1 优先权日:2000-05-22 标题:Thromboxane inhibitors, compositions and methods of use 发明人:TEJADA INIGO SAENZ DE 摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.
专利号:US-6469065-B1 优先权日:1996-02-02 标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use 发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
专利号:US-6436997-B1 优先权日:1998-06-01 标题 :Endogenous nitric oxide synthesis under conditions of low oxygen tension 发明人:DE TEJADA INIGO SAENZ 权利人:NITROMED INC 摘要:The present invention provides methods of promoting synthesis of nitric oxide or endothelium-derived relaxing factor (EDRF) in hypoxic mammalian tissues by administering at least one N-hydroxyguanidine compound that is a substrate of nitric oxide synthase, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides methods of promoting vasorelaxation and treating sexual dysfunctions in patients by administering at least one N-hydroxyguanidine compound that is a substrate for nitric oxide synthase, and, optionally, at least one vasoactive agent and/or thromboxane A2 receptor antagonist. The present invention also provides methods for treating clinical conditions resulting from hypoxic conditions such as pulmonary disease, cardiovascular disorders, circulatory hypoxia, specific organ hypoxia, localized hypoxia, edema, central nervous system disorders, memory loss, or arterial disease. The present invention also provides methods for treating clinical conditions resulting from an abnormally high level of arginase activity, such as, heart disease, systemic hypertension, pulmonary hypertension, sexual dysfunction, autoimmune disease, chronic renal failure and cerebral vasospasm. The present invention also provides methods for treating clinical conditions associated with a deficient nitric oxide pathway by administering at least one N-hydroxyguanidine compound and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists. The present invention also provides pharmaceutical compositions comprising at least one N-hydroxyguanidine compound, and, optionally, one or more vasoactive agents and/or thromboxane A2 receptor antagonists.
专利号:US-2014378538-A1 优先权日:2011-12-14 标 题:Methods of responding to a biothreat 发明人:BANCEL STEPHANE 权利人:MODERMA THERAPEUTICS INC 摘要:The present disclosure provides for devices, in particular mobile devices, which may be used in the synthesis of modified nucleic acid molecules, in particular modified mRNA molecules. The device for making the modified nucleosides, modified nucleotides and modified nucleic acids (e.g., mRNA) disclosed herein may be mobile devices comprising at least one sample block for insertion of one or more sample vessels, a device base with electronic control units for the sample block, a voltage supply, and one or more reagent(s) for the synthesis of at least one nucleic acid.
1: Tayeb BO, Eidelman A, Eidelman CL, McNicol ED, Carr DB. Topical anaesthetics for pain control during repair of dermal laceration. Cochrane Database Syst Rev. 2017 Feb 22;2:CD005364. doi: 10.1002/14651858.CD005364.pub3. Review. doi: 10.1002/14651858.CD010331.pub2. Review. doi: 10.4103/0970-9185.169049. Review. 4: Giordano D, Raso MG, Pernice C, Agnoletti V, Barbieri V. Topical local anesthesia: focus on lidocaine-tetracaine combination. Local Reg Anesth. 2015 Nov 27;8:95-100. doi: 10.2147/LRA.S41836. eCollection 2015. Review. 5: Beshay SM, Rivera G, Balthasar J, Florea N. Efficacy and Clinical Value of Commonly Used Ingredients in Pain Management Compounds: A LITERATURE REVIEW. Int J Pharm Compd. 2015 Jul-Aug;19(4):295-300. Review. doi: 10.1111/coa.12563. Epub 2016 Feb 11. Review. doi: 10.1007/s00540-015-2066-0. Epub 2015 Aug 25. Review. doi: 10.1016/j.jemermed.2015.06.069. Epub 2015 Aug 15. Review. doi: 10.1136/emermed-2014-204066. Epub 2014 Oct 28. Review. doi: 10.1016/j.jcrs.2014.08.001. Review. doi: 10.1002/14651858.CD004236.pub3. Review. Review. Review. Review. doi: 10.1016/j.ijporl.2012.05.022. Epub 2012 Jun 25. Review. doi: 10.1136/emermed-2012-201159.2. Review. doi: 10.3109/01480545.2011.653490. Epub 2012 Feb 24. Review. doi: 10.1111/j.1460-9592.2011.03769.x. Epub 2011 Dec 28. Review. doi: 10.1002/14651858.CD005364.pub2. Review. Update in: Cochrane Database Syst Rev. 2017 Feb 22;2:CD005364. pii: 0313. Review.
合成参考文献
参考文献:10.1007/s00228-010-0784-7 摘要:Chopade AR, Mulla WA. Novel strategies for the treatment of inflammatory hyperalgesia. European Journal of Clinical Pharmacology. 2010 Feb 13;66(5):429–44. doi: 10.1007/s00228-010-0784-7. 参考文献:10.1007/s00540-010-0889-2 摘要:Shiotsuka J, Sanui M, Lefor A. Safe use of landiolol hydrochloride in a patient with marked pseudocholinesterase deficiency. Journal of Anesthesia. 2010 Feb 13;24(2):309–10. doi: 10.1007/s00540-010-0889-2. 参考文献:10.1007/s00259-009-1376-6 摘要:Keijsers RG, Grutters JC, van Velzen-Blad H, van den Bosch JM, Oyen WJ, Verzijlbergen FJ. 18F-FDG PET patterns and BAL cell profiles in pulmonary sarcoidosis. European Journal of Nuclear Medicine and Molecular Imaging. 2010 Feb 16;37(6):1181–8. doi: 10.1007/s00259-009-1376-6. 参考文献:10.1021/ac902540b 摘要:Holman SW, Wright P, Langley GJ. A rapid methodology for the characterization of dialkyl tertiary amine-N-oxide metabolites using structurally dependent dissociation pathways and reconstructed ion current chromatograms. Anal Chem. 2010 Mar 15;82(6):2347–54. doi: 10.1021/ac902540b. 参考文献:10.2147/opth.s21247 摘要:Almubrad TM, Osuagwu UL, Alabbadi I, Ogbuehi KC. Comparison of the precision of the Topcon SP-3000P specular microscope and an ultrasound pachymeter. Clin Ophthalmol. 2011;5():871–6.