CAS: 171596-41-1; (1R,3R)-Methyl 1-(Benzo[d][1,3]Dioxol-5-yl)-2,3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indole-3-Carboxylate

上下游产品

CAS号120-57-0 胡椒醛 | CAS号14907-27-8 D-色氨酸甲酯盐酸盐 | CAS号4299-70-1 L-色氨酸甲酯 | CAS号171596-42-2 methyl (1S,3R)-... | CAS号67-56-1 甲醇 | CAS号1039484-71-3 (3R)-1-(3,4-met... | CAS号749864-17-3 methyl (R)-2-((... | CAS号153-94-6 D-色氨酸 | CAS号171489-59-1 (1R,3R)-1-(1,3-... | CAS号171596-27-3 12-表-他达拉非 | CAS号171596-36-4 去甲基他达那非 | CAS号171596-29-5 他达那非

胡椒醇置于manganese(Iv) Oxide体系中,用 二氯甲烷,异丙醇 用作溶剂,化学反应生成(1R,3R)-1,2,3,4-四氢-1-(3,4-亚甲基二氧基苯基)-9H-吡啶并[3,4-B]吲哚-3-羧酸甲酯
参考文献:支架探索对新型双重作用组蛋白脱乙酰酶和磷酸二酯酶5抑制剂治疗阿尔茨海默氏病的影响
标题:支架探索对新型双重作用组蛋白脱乙酰酶和磷酸二酯酶5抑制剂治疗阿尔茨海默氏病的影响
摘要:一种同时抑制磷酸二酯酶5(pde5)和组蛋白脱乙酰基酶(hdac)的新型系统治疗方法已被证实是治疗阿尔茨海默氏病(ad)的一种潜在的新型治疗策略.最近报道了带有西地那非核心的同类双重抑制剂,铅分子7已经在ad动物模型中证明了这种策略.由于脚手架可能在主要活动,Adme-Tox分析以及知识产权中发挥关键作用,因此我们探索了其他脚手架(基于vardenafil和tadalafil的核心),并评估了它们对关键参数(例如主要活动,渗透性,毒性和体内(海马的药代动力学和功能反应),以鉴定具有不同化学型的潜在替代铅分子,以进行体内测试.
Doi:10.1021/acschemneuro.6B00370

专利信息

专利号:US-2011105751-A1
优先权日:2008-03-31
标题:Conversion of tryptophan into beta-carboline derivatives
发明人：PIRC SAMO
权利人:LEAK PHARMACEUTICALS D D
摘要:The invention belongs in the field of organic chemistry and relates to a new shortened Pictet-Spengler type reaction for preparing isomerically pure β-carboline compounds useful for the synthesis of tadalafil.

专利号:US-2012123124-A1
优先权日:2011-04-22
标 题:Manufacturing process for Tadalafil from racemic or L-tryptophan
发明人：SOUKUP MILAN
权利人:SOUKUP MILAN; Drug Process Licensing Associates LLC
摘要:The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I, having (6R,12aR)-configuration, used for treatment of erectile dysfunction. Starting from racemic or L-tryptophan the invention describes preparation of an enantiomerically pure intermediate of formula II which is a known precursor in the synthesis of Tadalafil (formula I).

专利号:RU-2142463-C1
优先权日:1994-01-21
标题 :Tetracyclic derivatives, method of their synthesis (variants), pharmaceutical composition containing thereof and their use in therapy

专利号:US-8829023-B2
优先权日:2011-02-10
标题 :Process for obtaining compounds derived from tetrahydro-β-carboline
发明人：BERZOSA RODRÃ?GUEZ XAVIER; MARQUILLAS OLONDRIZ FRANCISCO
权利人:BERZOSA RODRÃ?GUEZ XAVIER; MARQUILLAS OLONDRIZ FRANCISCO; INTERQUIM SA
摘要:The invention relates to a process for obtaining compounds derived from tetrahydro-β-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.