专利号:US-5554725-A 优先权日:1994-09-14 标题:Synthesis of dolastatin 15 发明人:PETTIT GEORGE R 权利人:UNIV ARIZONA 摘要:The present invention relates to the synthesis of natural (-)- dolastatin and the elucidation of the absolute configuration of this important sea hare constituent. A segment synthetic strategy was utilized for obtaining the Dolabella auricularia (Indian Ocean sea hare) depsipeptide dolastatin 15. Reaction of protected (S)-Hiva-(S)-Phe (2c) with isopropenyl chloroformate followed by Meldrum's ester, cyclization (2c→3a) of the product in toluene and finally methylation afforded the key (S)-dolapyrrolidine (Dpy) derivative (3b). Condensation of tripeptide (8) with the three unit Dpy segment (5b) followed by deprotection and coupling (diethyl phosphorocyanidate) led to dolastatin 15 in 11% overall yield. The powerful and selective activity of dolastatin 15 against the U.S. National Cancer Institute's panel of human cell lines is reported.
专利号:US-7157477-B2 优先权日:2000-10-25 标题 :Aliphatic amino-substituted demethoxylated hypocrellins and their synthesis 发明人:ZHANG MANHUA; XU SHANGJIE; WU TAO; CHEN SHEN; SHEN TAO 权利人:INST OF PHOTOGRAPHIC CHEMISTRY 摘要:The invention involves a methods and compositions for use in photodynamic therapy. Novel perylenequinone derivatives, conjugates comprising perylenequinone derivatives and a binding agent, and methods of treatment using these compositions are disclosed. The present invention relates to the field of photosensitizers possessing photodynamic activities. They possess high photodynamic activities and low dark toxicities, which makes them as more potent photodynamic agents than HPD against cancer and AIDS virus.
专利号:US-5128489-A 优先权日:1989-10-05 标题:Process for production of optically active 2-(tetrahydropyran-2-yloxy)-1-propanol 发明人:KUMOBAYASHI HIDENORI; TACHIKAWA AKIO; OKEDA YOSHIKI; FUJIWARA TOSHIHIRO 权利人:TAKASAGO PERFUMERY CO LTD; DAIICHI SEIYAKU CO 摘要:A process for production of an optically active isomer of 2-(tetrahydropyran-2-yloxy)-1-propanol represented by formula (I): ##STR1## is disclosed, which comprises reacting an optically active isomer of a 1-acyloxy-2-propanol represented by formula (II): ##STR2## wherein R is a substituted or unsubstituted aryl group, with 3,4-dihydro-2H-pyran to obtain an optically active isomer of a 1-acyloxy-2-(tetrahydropyran-2-yloxy)propane represented by formula (III): ##STR3## wherein R is as defined above, and hydrolyzing the compound (III) to eliminate the acyl group. The optically active isomer of 2-(tetrahydropyran-2-yloxy)-1-propanol represented by formula (I) is an intermediate for synthesis of pyridobenzoxazine derivatives useful as a synthetic antibacterial agent, particularly an optically active isomer of ofloxacin.
专利号:US-9006347-B2 优先权日:2011-09-08 标 题 :Method of synthesising polycarbonates in the presence of a bimetallic catalyst and a chain transfer agent 发明人:WILLIAMS CHARLOTTE K; KEMBER MICHAEL; BUCHARD ANTOINE; JUTZ FABIAN 权利人:IMP INNOVATIONS LTD 摘要:The invention provides a process for the synthesis of a polycarbonate, the process comprising the step of reacting carbon dioxide with at least one epoxide in the presence of a catalyst of formula (I) and a chain transfer agent. The invention also provides a polymerization system for the copolymerization of carbon dioxide and at least one epoxide comprising a catalyst of formula (I) and a chain transfer agent, polycarbonates produced by the inventive process, a block copolymer comprising a polycarbonate produced by the inventive process, and a method of producing the block copolymer. The invention also relates to novel catalysts of formula (III).
专利号:US-6069243-A 优先权日:1998-10-06 标 题 :Process for oligonucleotide synthesis 发明人:SCOZZARI ANTHONY 权利人:ISIS PHARMACEUTICALS INC 摘要:The present invention describes methods for linking phosphoramidite nucleosides to a solid support-bound nucleoside. This invention presents novel processes for synthesizing oligonucleotides. Acetonitrile having a water content between 30 ppm and about 1250 ppm is used as the solvent for the washing steps in solid phase oligonucleotide synthesis, or is used as a solvent for the capping reagent or oxidizing reagent. The processes of the present invention are amenable to large-scale, economic oligonucleotide synthesis using the phosphoramidite method.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
[参考文献]: Irena Pulko, Et Al. Ultra-High Surface Area Functional Porous Polymers By Emulsion Templating And Hypercrosslinking: Efficient Nucleophilic Catalyst Supports. Chemistry. 2010 Feb 22;16(8):2350-4. [参考文献]: Tobias Rogosch, Et Al. Novel Bioactive Metabolites Of Dipyrone (Metamizol). Bioorg Med Chem. 2012 Jan 1;20(1):101-7.
合成参考文献
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