CAS: 465-21-4; 5-((3S,5R,8R,9S,10S,13R,14S,17R)-3,14-Dihydroxy-10,13-Dimethylhexadecahydro-1H-Cyclopenta[a]Phenanthren-17-yl)-2H-Pyran-2-One

上下游产品

(+)-digitoxigenin 5-(3'β-benzyloxy-14'-hydroxy-5'β,14'β-androstan-17'β-yl)-2H-pyran-2-one 2-mesitylenesulphonyl chloride 5-(3'β-benzyloxy-5'β-androst-14'-en-17'β-yl)-3,6-dihydro-2H-pyran-2,3-diol(3β,5β)-3-(acetyloxy)-14-hydroxy-bufa-20,22-dienolide 14-hydroxy-3β-(4-nitro-benzoyloxy)-5β,14β-bufa-20,22-dienolide 3β-hydroxy-21-nor-5β-pregnen-(14)-oic acid-(20) 12β-hydroxybufalin

📜在 三乙基硼,氧气,三正丁基氢锡,盐酸,水体系中,用 正己烷,二氯甲烷,甲醇 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,反应 24.0H,以73%的收率获得产物蟾毒灵
参考文献:五种丁二烯内酯的统一全合成
标题:五种丁二烯内酯的统一全合成
摘要:我们报告了五个bufadienolides的统一总合成:Bufalin(1),Bufogenin B(2),Bufotalin(3),Vulgarobufotoxin(4)和3-(n-琥珀酰精氨酰基)bufotalin(5).甾体abcd环8产生后,D环与2-吡喃酮部分交叉偶联并立体选择性环氧化反应生成6.tmsotf促进了立体定向的1,2-氢化物从6转变为19的β定向2-吡喃酮.从官能团操作19提供1-5,可有效抑制癌细胞的生长.
DOI:10.1021/acs.Orglett.0C03251

专利信息

专利号:US-3682895-A
优先权日:1970-07-17
标题 :Synthesis of 3-hydroxy-5-bufa-20,22-dienolide
发明人：PETTIT GEORGE R; FESSIER DYRAL C; PAUIL KENNETH D
权利人:GEORGE R PETTIT; DYRAL C FESSIER; KENNETH D PAUIL
摘要:THERE IS PROVIDED A NOVEL METHOD OF SYNTHEESIZING 5ABUFADIENOLIDES, WHICH ARE USEFUL INTERMEDIATES IN THE TOTAL SYNTHESIS OF BUFALIN, A CARDIAC ACTIVE COMPOUND. EPIANDROSTERONE ACETATE IS CONVERTED INTO 3B - ACETOXYL-5APREGNANE-21-AL WHICH UNDERGOES CHAIN EXTENSION TO METHYL 3B-ACETOXYL-20-FORMYL-21-NOR-5A-CHOLANATE WHICH IS RING CLOSED TO FORM THE 3B - ACETOXY-5-A-BUF-20(21)-ENOLIDE WHICH IS DEHYDROGENATED TO THE CORRESPONDING BUFADIENOLIDE.

专利号:US-12187735-B2
优先权日:2018-09-17
标 题:Matter of composition, synthesis, formulation and application of FL118 platform positions 7 and 9-derived analogues for treatment of human disease
发明人：LING XIANG; LI QINGYONG; LI FENGZHI
权利人:CANGET BIOTEKPHARMA LLC
摘要:Described herein, are the chemical synthesis, matter of compositions, formulation, function, methods and uses of the FL118 platform Positions 7 and/or 9-derived analogues for treating cancer or other human diseases. Compounds derived from chemical modifications of the FL118 platform are employed alone or in combination with other anti-cancer agents to preclude, eliminate or reverse cancer phenotypes. This invention intends to realize unique personalized cancer treatment (personalized precision medicine) through application of a series of structural relevant individual FL118 platform-derived analogues, which target multiple cellular human disease-relevant proteins and their signaling pathways.

专利号:US-2025092058-A1
优先权日:2018-09-17
标 题 :Matter of composition, synthesis, formulation and application of fl 118 platform positions 7 and 9-derived analogues for treatment of human disease
发明人：LING XIANG; LI QINGYONG; LI FENGZHI
权利人:CANGET BIOTEKPHARMA LLC
摘要:Described herein, are the chemical synthesis, compounds, methods and uses of the fluoroaryl-substituted derivatives at the FL118 position 7, which target multiple cellular human disease-relevant proteins and their signaling pathways.

专利号:US-9889182-B2
优先权日:2009-09-15
标 题 :Assisted enzyme replacement therapy
发明人：ESKO JEFFREY D; TOR YITZHAK
权利人:ESKO JEFFREY D; TOR YITZHAK; UNIV CALIFORNIA
摘要:Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.

专利号:US-3134772-A
优先权日:1961-05-01
标 题:Method of synthesis of bufalin
发明人：HEISABURO KONDO; SETSURO OHNO
权利人:HEISABURO KONDO; SETSURO OHNO

专利号:WO-2024109742-A1
优先权日:2022-11-21
标题:Method for efficiently synthesizing bufadienolides and derivatives thereof
发明人：LIN GUOQIANG; YE WENBO; ZHAO QUNFEI; ZHANG JIANGE; HE QINGLI; WANG CHAO; YU SHAOPENG
权利人:UNIV SHANGHAI TRADITIONAL CHINESE MEDICINE
摘要:Disclosed in the present invention is a method for efficiently synthesizing bufadienolides and derivatives thereof. By starting from cheap and easily-available androstenedione 4-AD, the method performs bio-enzyme oxidization on same to obtain 14-α-hydroxy-androstane-17-one compounds, then completes loading of E-ring pyrone by using chemical conversion without any protective group so as to obtain a key intermediate, and achieves synthesis of bufadienolides by starting from the key intermediate. The method synthesizes resibufogenin in just eight operation steps, has simple and short route, simple operations and large reaction scale, can be used for large-scale preparation of such natural products, and has use prospects in industrial production.