酒石酸肾上腺素置于ammonium Hydroxide体系中,用 水 作为反应溶剂,化学反应 3.0H,以93%的收率获得产物肾上腺素 参考文献: Process For The Preparation Of Optically Enriched Adrenaline[fr] Procédé De Préparation D'Adrénaline Enrichie Optiquement 标题: Process For The Preparation Of Optically Enriched Adrenaline[fr] Procédé De Préparation D'Adrénaline Enrichie Optiquement 摘要:提供了一种生产(-)-肾上腺素和(-)-肾上腺素-L-酒石酸盐的过程.该过程提供了一种新的,高效且商业可行的对消旋肾上腺素进行光学分辨的方法.在一个方面,提供了一种合成(-)-肾上腺素的一锅法过程.该过程提供了一种简单且成本较低的方法,可用于制备符合api质量标准的商业规模批次的(-)-肾上腺素和(-)-肾上腺素-L-酒石酸盐.该过程避免了使用昂贵且不可预测的手性催化剂.
专利号:US-6479549-B2 优先权日:2000-02-28 标 题:Carnosic acid derivatives for promoting synthesis of nerve growth factor 发明人:KOSAKA KUNIO; MIYAZAKI TOSHITSUGU; YOKOI TOSHIO 权利人:NAGASE & CO LTD 摘要:A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.
专利号:US-7692019-B2 优先权日:2000-12-04 标 题:Methods for the stereoselective synthesis of substituted piperidines 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
专利号:US-3846399-A 优先权日:1969-04-10 标题:Process for controlled stepwise synthesis of polypeptides 发明人:HIRSCHMANN R; DENKEWALTER R 权利人:MERCK & CO INC 摘要:The invention disclosed herein relates to a novel process for the controlled, stepwise synthesis of polypeptides and proteins. More particularly, it is concerned with a process for the rapid and efficient preparation of polypeptides in which multiple sequential steps are carried out without isolation of intermediate peptides. This process for the controlled stepwise synthesis of polypeptides involves reacting a starting amino acid or peptide (or derivative thereof) with an N-carboxy amino acid anhydride (or derivative thereof) in an aqueous medium under conditions of controlled pH such that the only amino group present in appreciable concentration in reactive form during the course of the reaction is the amino group in the starting amino acid or peptide.
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2008146656-A1 优先权日:2005-06-01 标题:Use of a steroid sulphatase inhibitor for inhibiting the synthesis of androstenedione and/or testosterone 发明人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 权利人:REED MICHAEL JOHN; PUROHIT ATUL; WOO LOK WAI LAWRENCE; POTTER BARRY VICTOR LLOYD 摘要:There is provided use of a compound capable of inhibiting a steroid sulphatase enzyme (E.C.3.1.6.2) in the manufacture of a medicament for inhibiting in vivo synthesis of at least one of androstenedione and testosterone, which may be useful for the treatment of hirsutism, excess sebum production, benign breast disease, benign ovarian disease, polycystic ovarian disease and female infertility among others.
专利号:US-6391344-B2 优先权日:1999-12-02 标题:Method of promoting synthesis of nerve growth factor 发明人:KOSAKA KUNIO; MIYAZAKI TOSHITSUGU; ITO HISATOMI 权利人:NAGASE & CO LTD 摘要:A method of promoting the synthesis of nerve growth factor comprising administering an effective amount of rosemary and/or sage extracts or carnosic acid and/or carnosol as an effective ingredient to a subject requiring such promotion. The present method can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.
1: Dos Reis Júnior A, Quinto D. Digital block with or without the addition of epinephrine in the anesthetic solution. Braz J Anesthesiol. 2016 Jan-Feb;66(1):63-71. doi: 10.1016/j.bjane.2013.12.004. Epub 2015 Nov 25. doi: 10.1177/1942602X15607604. doi: 10.1093/bja/aev422. doi: 10.1136/archdischild-2015-310092. Epub 2015 Nov 23. doi: 10.1097/AAP.0000000000000327. doi: 10.1016/j.ygcen.2015.10.015. Epub 2015 Nov 11. doi: 10.1097/CCM.0000000000001349. doi: 10.1016/j.hrthm.2015.08.021. Epub 2015 Aug 14. doi: 10.1109/JBHI.2014.2371533. Epub 2014 Nov 20. doi: 10.1016/j.ijcard.2015.11.182. Epub 2015 Dec 2. doi: 10.1007/978-3-319-20215-0_12. doi: 10.1016/j.ajem.2015.09.007. Epub 2015 Sep 21. doi: 10.1016/j.bjan.2013.12.004. Epub 2015 May 23. Portuguese. doi: 10.1016/j.otsr.2015.09.026. Epub 2015 Nov 6. doi: 10.1016/j.anai.2015.09.011. Epub 2015 Oct 12. doi: 10.1016/j.jcrc.2015.08.016. Epub 2015 Sep 1. doi: 10.1007/s00216-015-9066-7. Epub 2015 Oct 1.
合成参考文献
参考文献:10.1373/clinchem.2006.068445 摘要:Kushnir MM, Rockwood AL, Roberts WL, Pattison EG, Owen WE, Bunker AM, Meikle AW. Development and performance evaluation of a tandem mass spectrometry assay for 4 adrenal steroids. Clin Chem. 2006 Aug;52(8):1559–67. doi: 10.1373/clinchem.2006.068445. 参考文献:10.1093/hmg/8.13.2387 摘要:Blagitko N, Schulz U, Schinzel AA, Ropers HH, Kalscheuer VM. gamma2-COP, a novel imprinted gene on chromosome 7q32, defines a new imprinting cluster in the human genome. Hum Mol Genet. 1999 Dec;8(13):2387–96. doi: 10.1093/hmg/8.13.2387. 参考文献:10.1016/s0361-9230(02)00762-1 摘要:Lambert G, Naredi S, Edén E, Rydenhag B, Friberg P. Monoamine metabolism and sympathetic nervous activation following subarachnoid haemorrhage: influence of gender and hydrocephalus. Brain Res Bull. 2002 May;58(1):77–82. doi: 10.1016/s0361-9230(02)00762-1. 参考文献:10.1038/nn1296 摘要:Kaufer D, Ogle WO, Pincus ZS, Clark KL, Nicholas AC, Dinkel KM, Dumas TC, Ferguson D, Lee AL, Winters MA, Sapolsky RM. Restructuring the neuronal stress response with anti-glucocorticoid gene delivery. Nat Neurosci. 2004 Sep;7(9):947–53. doi: 10.1038/nn1296.