CAS: 477-47-4; (5R,5As,8Ar,9R)-9-Hydroxy-5-(3,4,5-Trimethoxyphenyl)-5,8,8A,9-Tetrahydrofuro[3',4':6,7]Naphtho[2,3-D][1,3]Dioxol-6(5Ah)-One

上下游产品

鬼臼毒素 Podofilox 518-28-5
5,8,8A,9-四氢-9-羟基-5-(3,4,5-三甲氧基苯基)-(5R,5Ar,8Ar,9S)-呋喃并[3',4':6,7]萘并[2,3-D]-1,3-二氧杂环戊烯-6(5Ah)-酮 Epipodophyllotoxin 09/07/4375
(+/-)-Epi-Picropodophyllin 477-47-4
4’-去甲鬼臼毒素 4-Demethylpodophyllotoxin 40505-27-9
4'-O-Demethylpicropodophyllotoxin 112066-16-7
8-Hydroxy-7-Hydroxymethyl-5-(3,4,5-Trimethoxy-Phenyl)-5,6,7,8-Tetrahydro-Naphtho[2,3-D][1,3]Dioxole-6-Carboxylic Acid 4354-75-0
(1R,2S,3R,4R)-4-O-(2-Trimethylsilylethoxy)Methylpicropodophyllin 261158-29-6
(+)-4-O-(Tert-Butyldimethylsilyl)Picropodophyllin 108448-52-8
Picropodophyllic Acid Hydrazide 78216-05-4
(5R)-5,8,8Ab,9-四氢-5B-(3,4,5-三甲氧基苯基)呋喃并[3',4':6,7]萘并[2,3-D]-1,3-二氧杂环戊烯-6(5Abh),9-二酮 (5Ar,8As,9R)-9-(3,4,5-Trimethoxyphenyl)-5A,6,8A,9-Tetrahydrofuro[3',4':6,7]Naphtho[2,3-D][1,3]Dioxole-5,8-Dione 477-48-5

鬼臼毒素置于sodium Acetate体系中,用 乙醇,水 作为反应溶剂,化学反应 12.0H,以78%的收率获得产物苦鬼臼毒素
参考文献:鬼臼毒素在乙醇中的热化学性质和热解产物抑制细胞生长活性的比较.
标题:鬼臼毒素在乙醇中的热化学性质和热解产物抑制细胞生长活性的比较.
摘要:缓冲乙醇溶液中的鬼臼毒素(1)通过两种途径降解.一个导致(a)鬼臼苦素(2),其经过脱水作用产生α-鬼臼苦素(5),后者重排得到β-鬼臼苦素(6),(b)鬼臼苦素的乙醚,8,和(c)表鬼臼毒素的乙醚7.另一种途径直接导致鬼臼毒素(10)和相应的乙醚9,并可能通过瞬时3,4-脱氢鬼臼毒素(5')导致β-鬼臼毒素(6).描述了这些化合物的1H NMR光谱,比较了它们的体外细胞抑制活性,并报道了它们的合成,包括鬼臼毒素乙基醚的合成.
DOI:10.1002/jps.2600751111

专利信息

专利号:US-6376676-B1
优先权日:1993-06-30
标题 :Intermediates in the synthesis of (±)-camptothecin and related compounds and synthesis thereof
发明人：CURRAN DENNIS P; LIU HUI
权利人:UNIV PITTSBURGH
摘要:The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (±)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

专利号:US-6252079-B1
优先权日:1993-06-30
标 题 :Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof
发明人：CURRAN DENNIS P; BOM DAVID
权利人:UNIV PITTSBURGH
摘要:The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursoris reacted with an aryl isonitrile having the formulawherein X is Br or I, and R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R16 is H, a C1-C6 alkoxy group, agroup wherein p is an integer between 4 and 12, or a C1-C12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

专利号:US-6982333-B2
优先权日:1993-06-30
标 题:Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof
发明人：CURRAN DENNIS P; JOSIEN HUBERT; KO SUNG BO
权利人:UNIV PITTSBURGH
摘要:The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-11311505-B2
优先权日:2017-02-24
标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
发明人：MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.