Bupivacaine N-Oxide置于盐酸,Titanium(III) Chloride体系中,用 甲醇,水,1,2-二氯乙烷,乙腈 用作溶剂,化学反应 2.0H,以62%的收率获得左布比卡因 参考文献: Selective Modification Of Organic Compounds In The Presence Of Amines And/or Sulfides[fr] Modification Sélective De Composés Organiques En Présence D'Amines Et/ou De Sulfures 标题: Selective Modification Of Organic Compounds In The Presence Of Amines And/or Sulfides[fr] Modification Sélective De Composés Organiques En Présence D'Amines Et/ou De Sulfures 摘要:本文揭示了一种用于选择性地修改含有胺,硫醚或胺和硫醚的有机化合物中可替代碳原子的方法.该方法利用了胺和硫醚的反应性,可以选择性地氧化形成在许多改性反应条件下是惰性的氧化物,并通过保护有机化合物中的胺,硫醚或胺和硫醚作为氧化物;将含氧化物的有机化合物置于适合进行改性反应的反应条件下;并使用还原剂去保护已修改的氧化物中的胺,硫醚或胺和硫醚,从而选择性地修改含有胺,硫醚或胺和硫醚的有机化合物中的可替代碳原子.
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-2023047214-A1 优先权日:2020-02-03 标题:Methods for microwave synthesis of degradable polymers for drug delivery 发明人:MURATOGLU ORHUN K; ORAL EBRU; GRINDY SCOTT 权利人:MASSACHUSETTS GEN HOSPITAL 摘要:Provided herein are methods of making degradable, additive-blended polymeric materials using microwave radiation and catalysts. The methods can include incorporation of therapeutic materials into the polymeric materials. There also are provided polymeric materials made by the methods and medical devices comprising the polymeric materials made by the methods.
专利号:WO-9628426-A1 优先权日:1995-03-10 标 题 :N-alkylpipecolic acid compounds, their preparation and use in the synthesis of levobupivacaine and analogues 发明人:DYER ULRICH CONRAD; ZAVAREH HOOSHANG SHAHRIARI 权利人:CHIROSCIENCE LTD; DYER ULRICH CONRAD; ZAVAREH HOOSHANG SHAHRIARI 摘要:Optically-enriched N,O-dialkyl pipecolates are useful in the preparation of levobupivacaine and related analgesics. They may be prepared simply by dialkylating optically-enriched pipecolic acid by reaction with an alkylating agent, in the presence of base and a polar aprotic solvent.
专利号:US-2015352230-A1 优先权日:2013-01-11 标 题:Synthesis and isolation of dendrimer based imaging systems 发明人:MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK 权利人:UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).
专利号:US-2012232225-A1 优先权日:2009-08-26 标 题:Synthesis and isolation of dendrimer systems 发明人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL 权利人:BAKER JR JAMES R; BANASZAK HOLL MARK M; MULLEN DOUGLAS GURNETT; ORR BRADFORD G; DESAI ANKUR; SANDER LEONARD M; WADDELL JACK NEEL; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis and isolation of dendrimer systems. In particular, the present invention is directed to novel dendrimer conjugates with defined and limited numbers of ligand conjugates and high levels of structural uniformity, methods of synthesizing the same, compositions comprising the conjugates, as well 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) diagnosis and/or therapy, pain therapy, etc.)).
专利号:US-9402911-B2 优先权日:2011-12-08 标题:Multifunctional small molecules 发明人:BAKER JR JAMES R; HUANG BAOHUA M; THOMAS THOMMEY P 权利人:UNIV MICHIGAN REGENTS 摘要:The present invention relates to dendrimer synthesis. Specifically, the present invention relates to dendrimer compositions (e.g., scaffolds) capable of copper-free click conjugation for use in the synthesis of functionalized dendrimers, and methods of use of the same.
1: Lv BS, Wang W, Wang ZQ, Wang XW, Wang JH, Fang F, Mi WD. Efficacy and safety of local anesthetics bupivacaine, ropivacaine and levobupivacaine in combination with sufentanil in epidural anesthesia for labor and delivery: a meta-analysis. Curr Med Res Opin. 2014 Nov;30(11):2279-89. doi: 10.1185/03007995.2014.946127. Epub 2014 Aug 5. Review. doi: 10.2165/11203250-000000000-00000. Review. Review. Japanese. Review. doi: 10.1097/ACO.0b013e32830c214c. Review. Review. German. Review. Review. Review. Review. Review. German. Review. Italian. Review. Review. Review. Review.
合成参考文献
参考文献:10.1111/j.1460-9592.2010.03259.x 摘要:Akin A, Ocalan S, Esmaoglu A, Boyaci A. The effects of caudal or intravenous clonidine on postoperative analgesia produced by caudal levobupivacaine in children. Paediatr Anaesth. 2010 Apr;20(4):350–5. doi: 10.1111/j.1460-9592.2010.03259.x. 参考文献:10.1111/j.1463-1318.2011.02721.x 摘要:Wolthuis AM, Penninckx F, Fieuws S, D'Hoore A. Outcomes for case-matched single-port colectomy are comparable with conventional laparoscopic colectomy. Colorectal Dis. 2012 May;14(5):634–41. doi: 10.1111/j.1463-1318.2011.02721.x. 参考文献:10.1007/s00101-011-1913-0 摘要:Geze S, Imamoğlu M, Cekic B. Awake caudal anesthesia for inguinal hernia operations: successful use in low birth weight neonates. Anaesthesist. 2011 Sep;60(9):841–4. doi: 10.1007/s00101-011-1913-0. 参考文献:10.1007/s10151-011-0720-6 摘要:Ozturk E, Yilmazlar A, Coskun F, Isik O, Yilmazlar T. The beneficial effects of preperitoneal catheter analgesia following colon and rectal resections: a prospective, randomized, double-blind, placebo-controlled study. Tech Coloproctol. 2011 Sep;15(3):331–6. doi: 10.1007/s10151-011-0720-6. 参考文献:10.1166/jnn.2011.4131 摘要:Wu RJ, Tsai TC, Luk HN, Chavali M. Fast detection of local anesthetic levobupivacaine by impedance method on PPy/SWCNT. J Nanosci Nanotechnol. 2011 Jun;11(6):4667–74. doi: 10.1166/jnn.2011.4131.