CAS: 6559-91-7; 4'-Demethylepipodophyllotoxin

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CAS号518-28-5 鬼臼毒素 | CAS号746639-24-7 (5R,5aR,8aR,9S)... | CAS号1185862-69-4 7-chlorodeoxypo... | CAS号64-19-7 冰醋酸 | CAS号33419-42-0 依托泊苷 | CAS号23363-35-1 木质素 P | CAS号127882-59-1 ethyl 4-[[(5R,9... | CAS号127882-83-1 (5S,5aR,8aR,9R)... | CAS号3590-93-0 4 ’-去甲去氧鬼臼毒素 | CAS号138355-94-9 (3aS,4S,9R,9aR)... | CAS号138456-91-4 (3aR,4S,9R,9aR)... | CAS号138355-95-0 ethyl 4-[[(3aS,... | CAS号125830-36-6 NPF-etoposide | CAS号138355-93-8 (3aS,4S,9R,9aR)...

依托泊苷置于三甲基氯硅烷,水,Barium Carbonate,Sodium Iodide体系中,用 丙酮,乙腈 作为反应溶剂,化学反应生成 4'-去甲基表鬼臼毒素
参考文献:新型带有4β-二硫键/三硫键作为细胞毒剂的鬼臼毒素衍生物的设计,合成和生物学评估†
标题:新型带有4β-二硫键/三硫键作为细胞毒剂的鬼臼毒素衍生物的设计,合成和生物学评估†
摘要:设计,合成了一系列新的含c-4β-二硫化物/三硫化物的鬼臼毒素衍生物,并对其生物学活性进行了评估,这些衍生物对人类癌细胞系(包括kb(口腔表皮癌细胞)和kb / Vcr(耐长春新碱的口腔))具有细胞毒活性.表皮癌细胞).这些化合物大多数显示出有希望的中等至非常好的细胞毒活性.特别地,它们中的一些表现出甚至优于依托泊苷的活性,特别是对于kb / Vcr细胞系,表明引入二硫化物/三硫化物部分将有利于克服依托泊苷的多药耐药性限制.此外,进一步对最有希望的化合物进行了代谢评估,结果表明二硫键在人体血浆中可以稳定8小时,体内抗癌活性.
DOI:10.1039/c5Ra12837D

专利信息

专利号:US-8148552-B2
优先权日:2007-09-25
标 题 :Process for the synthesis of anticancer (poly) aminoalkylaminoacetamide derivatives of epipodophyllotoxin
发明人：GUMINSKI YVES; GROUSSEAUD MARTIAL; IMBERT THIERRY
权利人:GUMINSKI YVES; GROUSSEAUD MARTIAL; IMBERT THIERRY; PF MEDICAMENT
摘要:The present invention describes a new process for the preparation of (poly)aminoalkylaminoacetamide compounds of epipodophyllotoxin useful for their applications in therapeutics as anticancer agents. This process comprises a step of condensation of a primary-amine-containing reactant, whose amine functions are not protected, with β-chloroacetamido-4′-epipodophyllotoxin in a polar aprotic organic solvent.

专利号:US-5086182-A
优先权日:1985-04-12
标题:Intermediates for the production of epipodophyllotoxin and related compounds and processes for the preparation and use thereof
发明人：VYAS DOLATRAI M; SKONEZNY PAUL M
权利人:BRISTOL MYERS CO
摘要:There is provided a novel and efficient stereoselective total synthesis of epiodophyllotoxin and related epipodophyllotoxin compounds of the general formula wherein R1 and R2 are independently hydrogen or (lower)-alkoxy, or R1 and R2, taken together, is methylenedioxy; R4 and R6 each are independently hydrogen or (lower) alkoxy; and R5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

专利号:US-4728740-A
优先权日:1985-04-12
标 题:Intermediates for the production of epipodophylotoxin and related compounds and processes for the preparation and use thereof
发明人：VYAS DOLATRAI M; SKONEZNY PAUL M
权利人:BRISTOL MYERS CO
摘要:There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula wherein R1 and R2 each are independently hydrogen or (lower)alkoxy, or R1 and R2, taken together, is methylenedioxy; R4 and R6 each are independently hydrogen or (lower)alkoxy; and R5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

专利号:US-5011948-A
优先权日:1985-04-12
标 题:Intermediates for the production of epipodophyllotoxin and related compounds and processes for the preparation and use thereof
发明人：VYAS DOLATRAI M; SKONEZNY PAUL M
权利人:BRISTOL MYERS CO
摘要:There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula wherein R1 and R2 each are independently hydrogen or (lower)alkoxy, or R1 and R2, taken together, is methylenedioxy; R4 and R6 each are independently hydrogen or (lower)alkoxy; and R5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

专利号:US-4122092-A
优先权日:1977-08-25
标 题:Total synthesis of (±)-picropodophyllone and (±)-4'-demethylpicropodophyllone
发明人：KENDE ANDREW S; RUTLEDGE PETER S
权利人:UNIV ROCHESTER
摘要:Efficient total syntheses of (±)-picropodophyllone and (±)-4'-demethylpicropodophyllone are described. These compounds are intermediates in the preparation of known antineoplastic agents.

专利号:US-5120862-A
优先权日:1985-04-12
标 题:Intermediates for the production of epipodophyllotoxin and related compounds and processes for the preparation and use thereof
发明人：VYAS DOLATRAI M; SKONEZNY PAUL M
权利人:BRISTOL MYERS CO
摘要:There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the and present invention wherein R1 and R2 each are independently hydrogen or (lower)alkoxy, or R1 ll and R2, taken together, is methylenedioxy; R4 and R6 each are independently hydrogen or (lower)alkoxy; and R5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present ivnention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.