N-(三氟乙酰基)-1-去甲基柔红霉素置于palladium Diacetate 4-二甲氨基吡啶,1,1'-Bis(Diphenylphosphino)Ferrocene,甲酸:三乙胺 1:1,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 吡啶,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 9.5H,反应生成 盐酸依达比星 参考文献:Method Of Producing 4-Demethoxydaunorubicin 标题:Method Of Producing 4-Demethoxydaunorubicin 摘要:本发明涉及一种合成4-去甲氧基多柔红霉素(伊达霉素)的方法,其化学结构如式(i),该方法涉及在软性lewis酸存在下对3'-Prot-多柔红霉素进行去甲基化.本发明的方法不包括在碳c7处断裂糖苷键,因此导致合成周期更快,最终产物的产率提高.
专利信息
专利号:US-4448724-A 优先权日:1982-12-20 标题 :Synthesis of 4-demethoxydaunomycinone 发明人:CAVA MICHAEL P; DOMINGUEZ DOMINGO 权利人:UNIV PENNSYLVANIA 摘要:A synthesis of 4-demethoxydaunomycinone and its derivatives from the known compound 9-acetyl-6,11-dihydroxy-7,8,9,10-tetrahydro-5,12-naphthacenedione. 4-Demethoxydaunomycinone may be converted to 4-demethoxydaunorubicin which is an anthracycline derivative known to have antitumor activity.
专利号:US-2025009786-A1 优先权日:2021-09-30 标 题 :Automated synthesis of polymeric dual drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
专利号:US-2010035799-A1 优先权日:2002-07-24 标 题:Method for the synthesis of anthracycline-peptide conjugates 发明人:FERNANDEZ ANNE-MARIE; DUBOIS VINCENT 权利人:UNIV CATHOLIQUE LOUVAIN; DIATOS SA 摘要:The present invention relates to a method for the preparation of a compound of formula (I) or pharmaceutically acceptable salts thereof and intermediates thereof, comprising the steps of: n n n n n n n n n n n n a) halogenating a compound of formula (II), resulting in compound of formula (IIa), n n n n n n n n n n n n n n n n b) reacting a compound of formula (IIa) at its 14 position with the thiol moiety of a peptide of formula (III), optionally in the presence of a suitable linker, to obtain said compound of formula (I), n n n n n n n n n n n n n n n n wherein R 1 represents OH, NH 2 or NH-peptide; R 2 represents H or —CO-peptide; R 3 represents OCH 3 , OH or H; R 4 represents H, or COCF 3 ; R 5 represents OH, O-tetrahydropyranyl or H; R 6 represents OH or H; R 7 represents H, OH, OCO(CH 2 ) 3 CH 3 or OCOCH(OC 2 H 5 ) 2 ; R 8 represents OH or H; R 9 represents OH or H; R 10 represents a halogen and L is an optional suitable linker arm.
专利号:US-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-2015158809-A9 优先权日:2013-02-26 标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds 发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P 权利人:XENOPORT INC 摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:US-2024350645-A1 优先权日:2021-07-22 标 题 :Automated synthesis of polymeric drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein L 1 , L 2 , L 3 , R 1 R 2 , M, p, q, m, and n are as defined herein. Additional compounds, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
1: Vigliotti ML, Dell'Olio M, La Sala A, Romano G, Tartarone A, Mele G, Musto C, Carella AM, Di Renzo N. Primary central nervous system lymphoma (PCNSL) in immunocompetent adults: analysis of a retrospective series of patients treated using idarubicin-containing regimen and radiotherapy. Hematol J. 2004;5(5):453-5. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review.
合成参考文献
摘要:S10 | SWISSPHARMA | Pharmaceutical List with Consumption Data | DOI:10.5281/zenodo.2623484