CAS: 471-95-4; (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3,14-Dihydroxy-10,13-Dimethyl-17-(2-Oxo-2H-Pyran-5-yl)Hexadecahydro-1H-Cyclopenta[a]Phenanthren-16-Yl Acetate

上下游产品

bufotalin 3-pimeloylarginine ester Epieti°Cholanolone5[(3S,5R,8R,9S,10S,13S)3hydroxy10,13dimethyl2,3,4,5,6,7,8,9,10,11,12,13dodecahydro1Hcyclopenta[a]phenanthren17yl]2Hpyran2one

📜雄烯二酮置于吡啶,咪唑,2,6-二甲基吡啶,甲醇,Sodium Tetrahydroborate,四(三苯基膦)钯,Palladium 10% On Activated Carbon,苯硅烷,氢气,氧气,Palladium Diacetate,Silica Gel,Sodium Carbonate,Potassium Tri-Sec-Butyl-Borohydride,氟化氢吡啶,Cobalt(II) Aceylacetonate,一水合肼,三乙胺,N,N-二异丙基乙胺,间氯过氧苯甲酸,Copper(L) Chloride,Lithium Chloride体系中,用 四氢呋喃,1,4-二氧六环,乙醇,二氯甲烷,二甲基亚砜,N,N-二甲基甲酰胺,乙腈 作为反应溶剂,-78.0~80.0 °C,101.33 Kpa 条件下,反应 243.67H,反应生成 蟾毒它灵
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-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: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.

专利号:CN-117597329-A
优先权日:2021-05-05
标题:Method for the catalytic synthesis of tryptamine and precursors thereof

专利号:WO-2020061106-A2
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

专利号:CA-3111403-A1
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