甲酸甲酯 反应生成氯甲酸氯甲酯 参考文献:Kling; Florentin; Lassieur,Comptes Rendus Hebdomadaires Des Seances De L'Academie Des Sciences,1919,Vol. 169,P. 1047 标题:Kling; Florentin; Lassieur,Comptes Rendus Hebdomadaires Des Seances De L'Academie Des Sciences,1919,Vol. 169,P. 1047
专利号:US-8653238-B2 优先权日:2006-02-27 标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers 发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R 权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR 摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:EP-2354120-A1 优先权日:2003-08-20 标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; YAO FENMEI; LUDWIKOW MARIA J; PHAN THU; PENG GE 权利人:XENOPORT INC 摘要:The present invention relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-tluorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The present invention also relates to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-fluorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.
专利号:US-6894173-B2 优先权日:1999-07-09 标 题 :Intermediates useful for synthesis of heteroaryl-substituted urea compounds, and processes of making same 发明人:ZHANG LIN-HUA; ZHU LEI 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar 1 , Ar 2 , L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
专利号:US-2021087191-A1 优先权日:2020-12-04 标 题 :SUBSTITUTED 3-ISOBUTYL-9,10-DIMETHOXY-1,3,4,6,7,11B-HEXAHYDRO-2H-PYRIDO[2,1-a]ISOQUINOLIN-2-OL COMPOUNDS, THEIR SYNTHESIS, AND USE THEREOF 发明人:MILLER DAVE ALAN; ELLENBERGER DANIEL J; GUNIC ESMIR; GIRARDET JEAN-LUC; SPANGENBERG ANGELA 权利人:DISPERSOL TECHNOLOGIES LLC 摘要:The invention relates to substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds, their synthesis, pharmaceutical compositions containing them, and methods of using them in the treatment of disorders benefiting from inhibition of vesicular monoamine transporter 2 (VMAT2).
专利号:US-11840582-B2 优先权日:2021-03-18 标 题:Synthesis method of cyclosporine derivatives 发明人:YANG ZHEN; ZHANG QINGZHOU; LI FENGXIA; JIANG CHONGGUO; GONG JIANXIAN; HUANG JUN; ZHANG WEIBIN 权利人:UNIV PEKING SHENZHEN GRADUATE SCHOOL 摘要:The present disclosure relates to a method of synthesizing cyclosporine derivatives. The method includes: providing a precursor fluid of the cyclosporine derivative, an alkaline fluid and a ClCH 2 OCOCl solution; premixing the precursor fluid and the alkaline fluid to obtain a premixed solution; feeding the premixed solution into a first reaction chamber, reacting to prepare a first reaction liquid; feeding the first reaction liquid into a second reaction chamber, reacting the first reaction liquid with a CO 2 fluid to prepare a second reaction liquid; and reacting the second reaction liquid with the ClCH 2 OCOCl solution.