专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
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-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
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.
专利号:US-2009253746-A1 优先权日:2005-11-14 标题 :Synthesis and Preparations of Intermediates and New Polymorphs Thereof Useful For The Preparation Of Donepezil Hydrochlcoride 发明人:SOLDEVILLA MADRID NURIA 权利人:SOLDEVILLA MADRID NURIA 摘要:The invention relates to an improved process for preparing 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyin-dan- 1 -one (a key intermediate in the synthesis of donepezil hydrochloride), crystalline polymorph forms of this key intermediate and their use thereof for producing donepezil hydrochloride. In particular, the invention provides an improved method for producing the intermediate 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyindan-1-one. The process includes reacting 5,6-dimethoxyin-dan- 1 -one with 1-benzylpiperidine-4-carbaldehyde using potassium hydroxide in an aqueous solvent. The aqueous solvent can be a mixture of an organic solvent and water Where the organic solvent is not miscible with water, the reaction may be performed in the presence of a phase transfer catalyst.
1: Cummings J, Lai TJ, Hemrungrojn S, Mohandas E, Yun Kim S, Nair G, Dash A. Role of Donepezil in the Management of Neuropsychiatric Symptoms in Alzheimer's Disease and Dementia with Lewy Bodies. CNS Neurosci Ther. 2016 Mar;22(3):159-66. doi: 10.1111/cns.12484. Epub 2016 Jan 18. Review. doi: 10.1358/dot.2015.51.10.2389166. Review. doi: 10.1111/ane.12386. Epub 2015 Feb 18. Review. doi: 10.3233/JAD-142268. Review. doi: 10.1093/geront/gnt055. Epub 2013 Jun 7. Review. doi: 10.1517/17425255.2014.915028. Epub 2014 Apr 30. Review. Review. Epub 2014 May 1. Review. doi: 10.3233/JAD-132690. Review. doi: 10.1111/cns.12076. Epub 2013 Mar 6. Review. Review. Japanese. doi: 10.1155/2013/925702. eCollection 2013. Review. 14: Cheewakriengkrai L, Gauthier S. A 10-year perspective on donepezil. Expert Opin Pharmacother. 2013 Feb;14(3):331-8. doi: 10.1517/14656566.2013.760543. Epub 2013 Jan 14. Review. doi: 10.1517/13543784.2013.750650. Epub 2012 Dec 9. Review. Review. Russian. doi: 10.3233/JAD-122140. Review. Epub 2013 Aug 5. Review. 19: Christensen DD. Higher-dose (23 mg/day) donepezil formulation for the treatment of patients with moderate-to-severe Alzheimer's disease. Postgrad Med. 2012 Nov;124(6):110-6. doi: 10.3810/pgm.2012.11.2589. Review. Review.
合成参考文献
参考文献:10.1007/bf03327445 摘要:Panza F, Solfrizzi V, Frisardi V, Imbimbo BP, Capurso C, D’Introno A, Colacicco AM, Seripa D, Vendemiale G, Capurso A, Pilotto A. Beyond the neurotransmitter-focused approach in treating Alzheimer’s Disease: drugs targeting β-amyloid and tau protein. Aging Clinical and Experimental Research. 2009 Dec;21(6):386–406. doi: 10.1007/bf03327445. 参考文献:10.2165/11204820-000000000-00000 摘要:Plosker GL, Gauthier S. Spotlight on cerebrolysin in dementia. CNS Drugs. 2010 Mar;24(3):263–6. doi: 10.2165/11204820-000000000-00000. 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:10.1016/j.encep.2009.02.004 摘要:Amara G, Saada W, Ben Nasr S, Ben Hadj Ali B. [Cholinesterase inhibitors and depression in the elderly]. Encephale. 2010 Feb;36(1):77–81. doi: 10.1016/j.encep.2009.02.004. 参考文献:10.1371/journal.pone.0020629 摘要:Arikawa M, Kakinuma Y, Handa T, Yamasaki F, Sato T. Donepezil, Anti-Alzheimer's Disease Drug, Prevents Cardiac Rupture during Acute Phase of Myocardial Infarction in Mice. PLoS ONE. 2011 Jul 05;6(7):e20629. doi: 10.1371/journal.pone.0020629.