专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-5220016-A 优先权日:1991-07-29 标 题:Synthesis of navelbine analogs 发明人:MAGNUS PHILIP D; THURSTON LEE S 权利人:UNIV TEXAS 摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.
专利号:US-5523411-A 优先权日:1994-03-14 标题 :Synthesis of mitomycin and its analogs 发明人:JIMENEZ LESLIE; WANG ZHENG 权利人:UNIV RUTGERS 摘要:The present invention relates to the synthesis of mitomycin and analogs thereof that are useful as anticancer antibiotics. The invention further relates to analogs of mitomycin, which can be prepared according to the methods of synthesis provided. The synthetic method of the invention provides for reacting a derivitized indole with a dialkylvinylsulfonium salt to yield a tricyclic skeleton having the precursors of the fourth ring in one step, followed by an oxidation step or steps to close the fourth ring and prepare mitomycin or a related compound.
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-2006183758-A1 优先权日:2005-02-17 标 题:Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans 发明人:BEARD CHARLES D; LEE VING J; WHITTLE C E 权利人:CB RES AND DEV INC 摘要:Methods of synthesis of intermediates that are useful as bioisosteres of the indole, benzofuran and benzothiophene scaffold are disclosed.
专利号:WO-9855532-A1 优先权日:1997-06-03 标题:Electrochemical synthesis of electrically conductive polymers and products thereof 发明人:KINLEN PATRICK J 权利人:ZIPPERLING KESSLER & CO 摘要:The electrochemical synthesis of electrically conductive polyaniline salts is provided. The method comprises electrochemical oxidation of an aromatic heterocyclic or aniline monomer oxidatively polymerizable to an intrinsically conductive polymer in the presence of water, an organic acid and, optionally, an organic solvent and an electron transfer mediator. Depending upon the water solubility of the organic acid, ICP salts soluble in either water or xylenes are produced.