📜4-Ethyl-5-Hydroxy-1-(4-Methoxybenzyl)-4-Methyl-3-(Methylthio)Pyrrolidin-2-One置于ammonium Cerium(Iv) Nitrate,Raney Nickel (W-2),Pyridinium Chlorochromate体系中,用 乙醇,二氯甲烷,水,乙腈 作为反应溶剂,化学反应 6.0H,反应生成 乙琥胺 参考文献:Uncatalyzed Cationic Olefin Cyclizations Of N-Vinylic α-Chloro-α-Thioacetamides. Formation Of β-And γ-Lactams 标题:Uncatalyzed Cationic Olefin Cyclizations Of N-Vinylic α-Chloro-α-Thioacetamides. Formation Of β-And γ-Lactams 摘要:N-Vinylic Alpha-Chloro-Alpha-Thioacetamides Were Found To Cyclize Without A Catalyst In Two Different Manners Depending Upon The Nature Of The Substituents At The Terminus Of The N-Vinylic Bond. Thus,Bis(Phenylthio)-Substituted Enamides 8A-C Cyclized In A 4-Exo-Trig Manner To Give 4-Methylene-Beta-Lactams 10A-C,Whereas Mono(Phenylthio)-,Monophenyl-,Diphenyl-,And Dialkyl-Substituted Congeners 23A,B,28,And 38 Cyclized In A 5-Endo-Trig Manner To Give Gamma-Lactams 26A,B,30,And 39,Respectively. The Product 38 Was Transformed Into An Anticonvulsant Agent Ethosuximide (42). DOI:10.1016/0040-4020(95)00056-E
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:US-2011040105-A1 优先权日:2008-04-16 标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine 发明人:HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL 权利人:ARENA PHARM INC 摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
专利号:US-7309799-B2 优先权日:2004-06-01 标 题:Methods for the synthesis of milnacipran and congeners thereof 发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V 权利人:COLLEGIUM PHARMACEUTICAL INC 摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
专利号:US-12201669-B2 优先权日:2021-03-11 标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology 发明人:TSAI LI-HUEI; BLANCHARD JOEL 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.
专利号:US-6030613-A 优先权日:1995-01-17 标题:Receptor specific transepithelial transport of therapeutics 发明人:BLUMBERG RICHARD S; SIMISTER NEIL E; LENCER WAYNE I 权利人:BRIGHAM & WOMENS HOSPITAL; UNIV BRANDEIS 摘要:The present invention relates in general to methods and products for initiating an immune response against an antigen, and in particular relates to transepithelial delivery of antigens to provoke tolerance and immunity. The present invention further relates to methods and products for the transepithelial delivery of therapeutics. In particular, the invention relates to methods and compositions for the delivery of therapeutics conjugated to a FcRn binding partner to intestinal epithelium, mucosal epithelium and epithelium of the lung. The present invention further relates to the synthesis, preparation and use of the FcRn binding partner conjugates as, or in, pharmaceutical compositions for oral systemic delivery of drugs and vaccines.
专利号:US-7749985-B2 优先权日:2006-09-15 标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use 发明人:GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE 权利人:XENOPORT INC 摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.
1: Gören MZ, Onat F. Ethosuximide: from bench to bedside. CNS Drug Rev. 2007 Summer;13(2):224-39. Review. Review. Review. Review. Update in: Cochrane Database Syst Rev. 2005;(4):CD003032. Review. Review. Review. Japanese. Review. Review. Review.
合成参考文献
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