CAS: 14198-59-5; (2S,3R,11Bs)-2-[[(1R)-6,7-Dimethoxy-1,2,3,4-Tetrahydroisoquinolin-1-Yl]Methyl]-3-Ethyl-9,10-Dimethoxy-2,3,4,6,7,11B-Hexahydro-1H-Benzo[a]Quinolizine,Hydrochloride

📜(S)-Tert-Butyl 1-Allyl-6,7-Dimethoxy-3,4-Dihydroisoquinoline-2(1H)-Carboxylate置于四氢吡咯,吡啶,Rucl2(1,3-Dimesityl-Imidazolidin-2-yl)(Pcy3)(=chph),盐酸,Sodium Tetrahydroborate,Copper(L) Iodide,[(1S,2S)-N-(P-Toluensulfonyl)-1,2-Diphenylethanediamine](P-Cymene)Ruthenium (I),甲酸,20% Palladium Hydroxide-Activated Charcoal,水,氢气,三甲基乙酰氯,三乙胺,Potassium Hydroxide,Sodium Hydroxide,三氯氧磷体系中,用 四氢呋喃,甲醇,氘代二甲亚砜,乙醇,水,乙酸乙酯,乙腈,叔丁醇 用作溶剂,化学反应 81.02H,反应生成盐酸吐根碱
参考文献:(−)-Emetine 的高效且可扩展的不对称全合成,具有医药级品质;第一次多字母表合成
标题:(−)-Emetine 的高效且可扩展的不对称全合成,具有医药级品质;第一次多字母表合成
摘要:(−)-Emetine 的可扩展不对称全合成已经完成,Emetine 是一种来自吐根物种的天然产物生物碱,也是催吐剂中使用的吐根糖浆中的主要活性成分之一.该合成路线共有 13 个高效化学反应步骤,包括催化不对称烯丙基化和脂肪族化合物的工业脱氧,无需任何色谱纯化.(−)-Emetine.2Hcl 以 12% 的总收率和超过 93.2% 的 HPLC 纯度获得.该合成很容易放大到 237.1 克,应该可以为正在进行的药物开发生产更大数量的化合物,而该化合物目前以天然吐根糖浆的形式提供用于临床.
Doi:10.1021/acs.Oprd.2C00355

专利信息

专利号:US-9409879-B2
优先权日:2011-03-29
标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
发明人：DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA
权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT
摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

专利号:US-5981284-A
优先权日:1994-08-16
标 题 :Technique for acceleration of apoptotic cell death
发明人：NAMIKI HIDEO; KURITA TAKESHI
权利人:DISCOVISION ASS
摘要:A first embodiment of a cell culture system has a cell death accelerator comprising one or more cell death inducing substances, including serum albumin, hemoglobin, glycine and glutamic acid. In a second embodiment a cell death inhibitor comprises one or more kinds of cell death inhibiting substances which include mercapto group containing amino acids, other mercapto group containing compounds and tryptophan. In a third embodiment a cell death inhibitor comprises an inhibitor of RNA or protein synthesis, optionally augmented with a thiol. The system can be applied to selectively induce death of cultured cells, such as neoplastic cell lines, or to inhibit death of other cells, such as neoplastic cell lines or non-neoplastic cells such as brain cells.

专利号:US-2014121238-A1
优先权日:2011-03-29
标 题:Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents

专利号:US-3649641-A
优先权日:1969-11-04
标 题 :4-hydroxy - 1 - substituted-1h-thieno(2 3-c) pyrazole-5-carboxylic acid derivatives and intermediates thereto
发明人：KIM DONG H; SANTILLI ARTHUR A
权利人:AMERICAN HOME PROD
摘要:4 - HYDROXY-1-SUBSTITUTED-1H-THIENO(2,3-C)-PYRAZOLE-5CARBOXYLIC ACID DERIVATIVES USEFUL AS ANTIAMEBIC AGENTS ARE DISCLOSED, AS WELL AS METHODS OF SYNTHESIS OF THESE COMPOUNDS.

专利号:WO-2012131010-A1
优先权日:2011-03-29
标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents

专利号:EP-2691372-A1
优先权日:2011-03-29
标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents