CAS: 38390-45-3; 3',4'-Anhydrovinblastine

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CAS号71486-22-1 长春瑞滨 | CAS号363623-08-9 (S)-tert-Butyl ... | CAS号23360-92-1 长春罗新

(3Ar,3A1R,4R,5S,5Ar,10Br)-Methyl 4-Acetoxy-3A-Ethyl-9-((3R,5S,7R,9S)-5-Ethyl-5-Hydroxy-9-(Methoxycarbonyl)-2,4,5,6,7,8,9,10-octahydro-1H-3,7-Methano[1]Azacycloundecino[5,4-B]Indol-9-yl)-5-Hydroxy-8-Methoxy-6-Methyl-3A,3A1,4,5,5A,6,11,12-octahydro-1H-Indolizino[8,1-Cd]Carbazole-5-Carboxylate Sulfuric Acid置于盐酸,Iron(Iii) Chloride,沙丁胺醇,Ammonium Hydroxide,Sodium Tetrahydroborate,氯化铵体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 0.84H,反应生成 脱水长春碱
参考文献:一种酒石酸长春瑞滨的制备方法
标题:一种酒石酸长春瑞滨的制备方法
摘要:本发明公开了一种酒石酸长春瑞滨的制备方法,包括:1)脱水长春碱制备步骤:以硫酸长春质碱和文多灵为起始原料,经三氯化铁催化和硼氢化钠还原,得到脱水长春碱;2)溴代脱水长春碱制备步骤:脱水长春碱与n‑溴代琥珀酰亚胺进行溴代反应,得到溴代脱水长春碱粗品;溴代脱水长春碱粗品经过柱纯化,提高其纯度,得到溴代脱水长春碱;3)长春瑞滨制备步骤:溴代脱水长春碱与四氟硼酸银水溶液进行脱溴重排,得到长春瑞滨粗品;长春瑞滨粗品经过重结晶,得到长春瑞滨纯品;4)酒石酸长春瑞滨制备步骤:长春瑞滨纯品与酒石酸进行成盐反应,得到酒石酸长春瑞滨.本发明操作简单,副反应少,大大提高了纯度和收率,降低了生产成本,适合规模化生产.

专利信息

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-RE37449-E
优先权日:1987-02-06
标题:Process of synthesis of 3′,4′-anhydrovinblastine, vinblastine and vincristine
发明人：KUTNEY JAMES P; CHOI LEWIS S L; NAKANO JUN; TSUKAMOTO HIROKI; BOULET CAMILLE A; MCHUGH MICHAEL
权利人:UNIV BRITISH COLUMBIA
摘要:The present invention relates to the synthesis of dimer alkaloid compounds, particularly those of the Catharantus (Vinca) family, from an indole unit, such as cantharanthine, and a dihydroindole unit, such as vindoline. A multi-step process is disclosed including the steps of (1) of 1,4-reduction of a first dimeric iminium intermediate to an enamine compound by reaction with a 1,4-dihydropyridine compound; (2) oxidative transformation of the resulting enamine to a second iminium intermediate under controlled aeration; (3) reduction of the second iminium intermediate to form the target dimer alkaloid compounds. The entire process can be conducted in a one-pot operation to obtain the target compounds without isolation of the intermediates.

专利号:US-4305875-A
优先权日:1978-12-08
标 题 :Process for the synthesis of vinblastine and leurosidine
发明人：POTIER PIERRE; MANGENEY PIERRE; LANGLOIS NICOLE; LANGLOIS YVES
权利人:ANVAR
摘要:The invention provides a process for the preparation of leurosidine or vinblastine, which comprises hydroxylating and reducing DELTA 20' dehydroxy-20' vincaleucoblastine corresponding to formula (II): II

专利号:US-2011104052-A1
优先权日:2007-12-03
标 题 :Methods of synthesis and use of chemospheres
发明人：BARNETT BRADLEY POWERS; GESCHWIND JEFFREY
权利人:UNIV JOHNS HOPKINS
摘要:The present invention provides, in general, compositions comprising a hydrogel and an agent, for example a therapeutic agent or an imaging agent, for locoregional delivery. In certain preferred embodiments of the invention, the hydrogel compositions are detectable by Magnetic Responance and CT Scan and are used for locoregional delivery of therapeutic agents, for example chemotherapeutic agents. The invention also features polymer matrix compositions comprising nanoparticles that can be loaded after polymerization with bioactive agents, for example a diagnostic agent or therapeutic agent.

专利号:US-5034320-A
优先权日:1987-03-31
标题 :Vinblastine synthesis
发明人：ENDO TSUYOSHI
权利人:ALLELIX INC
摘要:The reaction of 3',4'-anhydrovinblastine with a Catharanthus roseus-derived protein fraction to form vinblastine is improved by conducting the reaction in the presence of a reducing agent such as the enzyme cofactor NADH. A cationic species such as manganous ion may also be added to the reaction. Vinblastine yields are enhanced.

专利号:US-9585890-B2
优先权日:2012-09-26
标题 :Modulators of androgen synthesis
发明人：DILLY SUZANNE; STOLOFF GREGORY; TAYLOR PAUL
权利人:TANGENT REPROFILING LTD
摘要:The present specification discloses compositions comprising at least one therapeutic compound capable of modulating androgen production and methods and uses for treating a disorder associated with androgen production using such compositions and/or compounds.