(1'R,6R,6Ar,7R,13S,14R,16R)-5-(Acetyloxy)-3',4',6,6A,7,13,14,16-octahydro-6'-Hydroxy-7',9-Dimethoxy-8-(Methoxymethoxy)-4,10,23-Trimethyl-19-Oxo-Spiro[6,16-(Epithiopropanoxymethano)-7,13-Imino-12H-1,3-Dioxolo[7,8]Isoquino[3,2-B][3]Benzazocine-20,1'(2'H)-Isoquinoline]-14-Carbonitrile置于三氟乙酸,Silver Nitrate体系中,用 四氢呋喃,水,乙腈 用作溶剂,化学反应 34.0H,反应生成他比特啶 参考文献: Process For The Preparation Of Ecteinascidin Derivative And Its Intermediate[fr] Procédé De Préparation D'Un Dérivé D'Ectéinascidine Et De Son Intermédiaire 标题: Process For The Preparation Of Ecteinascidin Derivative And Its Intermediate[fr] Procédé De Préparation D'Un Dérivé D'Ectéinascidine Et De Son Intermédiaire 摘要:本发明涉及一种改进的,工业上可行的trabectedin制备过程.本发明还涉及一种改进的,工业上可行的公式-A的trabectedin中间化合物制备过程.本发明使用成本更低的试剂,溶剂,并且工艺条件可以很容易地适用于商业规模.
专利信息
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-7820838-B2 优先权日:2002-01-29 标 题:Method for total synthesis of ecteinascidins and intermediate compounds thereof 发明人:FUKUYAMA TOHRU; KAN TOSHIYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R 2 of N 12 site is trichloroethoxycarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:WO-2007087220-A3 优先权日:2006-01-25 标题:The total synthesis of ecteinascidin 743 and derivatives thereof 发明人:DANISHEFSKY SAMUEL J; CHAN COLLIN 权利人:UNIV COLUMBIA; DANISHEFSKY SAMUEL J; CHAN COLLIN 摘要:This invention provides a method of synthesizing ecteinascidin 743 and derivatives. This invention also provides intermediate compounds and methods of treating tumors.
专利号:US-9227948-B2 优先权日:2012-06-19 标题:Process for the preparation of 2-substituted-2-(6-(substituted)-7-methylbenzo[D][1,3]dioxol-4-yl)acetic acid derivatives 发明人:MUDDASANI PULLA REDDY; CHINTALAPUDI MANIKUMAR; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD 摘要:Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I the above Formula I, XII, XIII, XV, wherein R 1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R 2 is C 1 -C 6 alkyl. 2,4-Dihydroxy-3-methylbenzaldehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin.
1: Trabectedin: Reimbursement Recommendation [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2025 Oct. Report No.: PX0377. 2025 Sep. Report No.: PX0377r. 18:2021-2032. doi: 10.2147/DDDT.S451223. 4: Povo-Retana A, Landauro-Vera R, Alvarez-Lucena C, Cascante M, Boscá L. Trabectedin and Lurbinectedin Modulate the Interplay between Cells in the Tumour Microenvironment-Progresses in Their Use in Combined Cancer Therapy. Molecules. 2024 Jan 9;29(2):331. doi: 10.3390/molecules29020331. Erratum in: Molecules. 2025 Jun 05;30(11):2472. doi: 10.3390/molecules30112472.
合成参考文献
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from 参考文献:10.1021/bi960306b 摘要:Pommier Y, Kohlhagen G, Bailly C, Waring M, Mazumder A, Kohn KW. DNA sequence- and structure-selective alkylation of guanine N2 in the DNA minor groove by ecteinascidin 743, a potent antitumor compound from the Caribbean tunicate Ecteinascidia turbinata. Biochemistry. 1996 Oct 15;35(41):13303–9. doi: 10.1021/bi960306b. 参考文献:10.1021/jm990241l 摘要:Zewail-Foote M, Hurley LH. Ecteinascidin 743: a minor groove alkylator that bends DNA toward the major groove. J Med Chem. 1999 Jul 15;42(14):2493–7. doi: 10.1021/jm990241l. 参考文献:10.1073/pnas.0510909103 摘要:Newman JC, Bailey AD, Weiner AM. Cockayne syndrome group B protein (CSB) plays a general role in chromatin maintenance and remodeling. Proc Natl Acad Sci U S A. 2006 Jun 20;103(25):9613–8.