专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:US-4354972-A 优先权日:1981-06-29 标 题 :Synthesis of steroids 发明人:KAISER EMIL T 权利人:KAISER EMIL T 摘要:This invention relates to the synthesis of steroids which are useful for their biological activity or which may be converted to steroids which have such activity. These syntheses include the steroid compounds and processes for their preparation. n An object of the invention is to provide syntheses which are applicable to materials which are readily available in good supply for converting such materials to steroids which are useful and desirable in the manufacture of pharmaceutical products. n More particularly, I have sought to discover processes and intermediate compounds useful in the synthesis of 24, 25-dihydroxycholesterol from hyodeoxycholic acid or lithocholic acid which are constituents of, and readily available from, animal bile.
专利号:WO-2025104679-A1 优先权日:2023-11-16 标题 :Processes for making intermediates for isoindolinone inhibitors of the mdm2-p53 interaction having anticancer activity 发明人:SHAKYA SAGAR; JOHNSON MATT; WONG NICHOLAS; BODHURI PRABHUDAS; DAVAR NIPUN 权利人:OTSUKA PHARMA CO LTD 摘要:The present disclosure relates to processes for preparing synthetic intermediates for the synthesis of isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity.
专利号:US-8026349-B2 优先权日:2004-08-20 标题 :Polynucleotide synthesis labeling chemistry 发明人:HARTSEL STEPHANIE A; KAISER ROBERT J; DELANEY MICHAEL O 权利人:DHARMACON INC 摘要:Methods and compositions for making nucleoside phosphoramidites and nucleic acids, including mono-, di-, and polynucleotides, comprising a linker covalently attached to a levulinyl moiety are provided. A levulinyl-protected linking moiety affords an orthogonal approach to modifying a polynucleotide during or after solid phase synthesis with a molecule of interest, for example, a conjugate or a dye.
专利号:US-6004965-A 优先权日:1994-12-20 标题 :Sulfonamides 发明人:BREU VOLKER; BURRI KASPAR; CASSAL JEAN-MARIE; CLOZEL MARTINE; HIRTH GEORGES; LOEFFLER BERND-MICHAEL; MUELLER MARCEL; NEIDHART WERNER; RAMUZ HENRI 权利人:HOFFMANN LA ROCHE 摘要:Compounds of the formula: ##STR1## where A, B, R 1 -R 8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
专利号:WO-2004046105-A2 优先权日:2002-11-15 标题 :Synthesis of 3,5-dihydroxy-7-pyrrol-1-yl heptanoic acids
[参考文献]: D C Landrum, Et Al. Gas-Liquid Chromatography-Mass Spectrometry Of Mono- And Dithiols As Their Tert.-Butyldimethylsilyl Derivatives. J Chromatogr. 1989 Dec 8:483:21-32. [参考文献]: O Breuer, Et Al. Use Of An 18O2 Inhalation Technique And Mass Isotopomer Distribution Analysis To Study Oxygenation Of Cholesterol In Rat. Evidence For In Vivo Formation Of 7-Oxo-, 7 Beta-Hydroxy-, 24-Hydroxy-, And 25-Hydroxycholesterol. J Biol Chem. 1995 Sep 1;270(35):20278-84.
合成参考文献
摘要:Tamao, K.; Kawachi, A., Science of Synthesis, (2002) 4, 455.