专利号:US-RE41366-E 优先权日:2001-06-15 标 题 :Total synthesis of galanthamine, analogues and derivatives thereof 发明人:THAL CLAUDE; GUILLOU CATHERINE; BEUNARD JEAN-LUC; GRAS EMMANUEL; POTIER PIERRE 权利人:CT NAT DEL LA RECH SCIENT CNRS 摘要:The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R 1 =a hydrogen atom, R 2 =a hydroxy group, R 1 and R 2 together form â•?O, R 3 , R 4 , and R 5 independently=a hydrogen atom, a hydroxy group or a (C 1 -C 2 )alkoxy group, R 6 â•?H, (C 1 -C 12 )alkyl, (CH 2 ) n NR 7 R 8 , or —(CH 2 ) n N + R 7 R 8 R 9 where n=1 to 12, Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a —SO, —SO 2 , or —NR 6 group where R 6 is as defined above or is an amine protecting group.
专利号:US-8450365-B2 优先权日:2009-05-12 标 题 :Efficient synthesis of galanthamine 发明人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ 权利人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ; UNIV TEXAS 摘要:The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
专利号:WO-2006046096-A3 优先权日:2004-08-16 标 题 :A polymorphic form of narwedine and its use in the synthesis of galantamine 发明人:LAHIRI SASWATA; PRASAD MOHAN; MAHESHWARI NITIN; KUMAR YATENDRA 权利人:RANBAXY LAB LTD; LAHIRI SASWATA; PRASAD MOHAN; MAHESHWARI NITIN; KUMAR YATENDRA 摘要:The present invention relates a polymorphic form of narwedine (Form B) and processes for the preparation thereof. Also provided is a process for the synthesis of galantamine using a polymorph of narwedine (Form B).
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-2009247754-A1 优先权日:2008-03-25 标 题:Method of preparing huperzine a and derivatives thereof 发明人:UNDERINER GAIL; GIBSON FRANK; HE LINLI; MEERA HARIHARA SUBRAMANIAN; GNANADEEPAM JESUDOSS MERCY; SAIGANESH RAMANATHAN; TUDHOPE STEPHEN R; AZADI-ARDAKANI MANOUCHEHR 权利人:DEBIOPHARM SA 摘要:The present invention is related to the synthesis of huperzine A. The synthesis includes a variety of process steps that increase productivity, reduce safety concerns, and allow for increasing production of compounds of desired optical isomer. The inventive methods may encompass a single improved reaction step that may be incorporated into a known reaction process for synthesizing huperzine A or a derivative thereof to improve the overall reaction. The inventive methods also encompass complete synthesis methods for preparing huperzine A or a derivative thereof.
专利号:US-9981949-B2 优先权日:2008-12-01 标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:OYSTER POINT PHARMA INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
1: Agrawal M, Saraf S, Saraf S, Antimisiaris SG, Chougule M, Shoyele SA, Alexander A. Nose-to-brain drug delivery: An update on clinical challenges and progress towards approval of anti-Alzheimer drugs. J Control Release. 2018 May 14. pii: S0168-3659(18)30268-2. doi: 10.1016/j.jconrel.2018.05.011. [Epub ahead of print] Review. doi: 10.3389/fpsyt.2018.00091. eCollection 2018. Review. 3: Tammenmaa-Aho I, Asher R, Soares-Weiser K, Bergman H. Cholinergic medication for antipsychotic-induced tardive dyskinesia. Cochrane Database Syst Rev. 2018 Mar 19;3:CD000207. doi: 10.1002/14651858.CD000207.pub2. Review. doi: 10.1080/14756366.2018.1443326. Review. doi: 10.2174/1874104501812010023. eCollection 2018. Review. 6: Khoury R, Rajamanickam J, Grossberg GT. An update on the safety of current therapies for Alzheimer's disease: focus on rivastigmine. Ther Adv Drug Saf. 2018 Mar;9(3):171-178. doi: 10.1177/2042098617750555. Epub 2018 Jan 8. Review.
合成参考文献
摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484