CAS: 475-81-0; (S)-1,2,9,10-Tetramethoxy-6-Methyl-5,6,6A,7-Tetrahydro-4H-Dibenzo[de,G]Quinoline

上下游产品

(+/-)-glaucine (S)-laudanosine diazomethane phenyltrimethylammonium chloride(+)-thalicmidine glaucine N-oxide thaliporphine 1,2,9,10-tetramethoxy-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline

醛基去甲海罂粟碱置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.0H,以84%的收率获得产物海罂粟碱
参考文献:酞菁吗啡n-同源物的半合成和心肌活性
标题:酞菁吗啡n-同源物的半合成和心肌活性
摘要:从有效成分phoebe Formosana中存在的丰富的磷化氢月桂氨酸(1)开始制备一种有效的抗心律不齐药物thaliporphine(5A)的n同源物和旋光异构体.用90%的h 2 So 4处理n-丙基去甲月桂氨酸产生了另一种产物,即11-磺酰基-1,11-脱水吗啡.的反应ñ-Formylnorglaucine(3A)与90%h 2 So 4,但是,得到的9-磺酰基-开环产物,为主要产物.用98%h 2 So 4处理3A产生了潘考丁(10),其在催化氢化后产生(+/-)-野烟碱.1 H NMR光谱分析已成功应用于监测晶体盐的光学纯度,同时进行了光学拆分.thaliporphine(5A)被证明比左侧的旋光异构体具有更好的正性变力作用和负的变时性作用,并且在制备的n同源物中对大鼠心脏组织表现出最佳活性.
DOI:10.1021/np3007765

专利信息

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-11612556-B2
优先权日:2014-12-16
标 题:Peptidic compounds, compositions comprising them and uses of said compounds, in particular cosmetic uses
发明人：PESCHARD OLIVIER; DOUCET ANNE; LEROUX RICHARD; MONDON PHILIPPE
权利人:SEDERMA SA
摘要:The peptidic compound comprises at least an aminoacid which is lysine, ornithine, diaminopropionic acid or diaminobutyric acid or a derivative of these aminoacids, on which a carboxylic acid is grafted via a peptidic bound on the nitrogen of the lateral chain, said carboxylic acid comprising a (poly)cycle or (poly)heterocycle. Preferably, the grafted carboxylic acid is an aminoacid or a derivative, in particular selected from, a proline, a hydroxyproline or pyroglutamic acid.The peptidic compound can stimulate the synthesis of the main molecules constituting the extracellular matrix of the skin, especially collagen 1 and 4 and elastin. It can be used for topical cosmetic treatment such as a global anti-aging treatment, or for specific activities, including anti-wrinkles, moisturizing, to improve the mechanical properties of the skin, firmness/tone/elasticity/flexibility, to increase density and volume of the skin, improve skin radiance, for a restructuring effect and/or to fight stretch marks.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-11617758-B2
优先权日:2009-12-31
标 题 :Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:MARIUS PHARMACEUTICALS LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-2013303495-A1
优先权日:2009-12-31
标题:Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:WO-2009035652-A1
优先权日:2007-09-13
标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof