CAS: 59379-02-1; Tert-Butyl 3-Formylpyrrolidine-1-Carboxylate

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CAS号114214-69-6 1-B°C-3-羟甲基吡咯烷 | CAS号201230-82-2 carbon monoxide | CAS号73286-71-2 N-B°C-2-吡咯啉 | CAS号73286-70-1 N-B°C-3-吡咯啉 | CAS号85310-69-6 吡咯烷-3-基甲醇 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号287193-00-4 1-B°C-3-炔基吡咯烷 | CAS号753015-96-2 1-B°C-3-乙烯基吡咯烷 | CAS号114214-69-6 1-B°C-3-羟甲基吡咯烷 | CAS号270912-72-6 1-B°C-3-(氨甲基)吡咯烷

1-Boc-3-羟甲基吡咯烷置于戴斯-马丁氧化剂体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.0H,反应生成 1-Boc-3-吡咯烷甲醛
参考文献:X 射线结构引导发现一种有效的口服生物可利用双人吲哚胺/色氨酸 2,3-双加氧酶 (Hido/htdo) 抑制剂,该抑制剂在帕金森病小鼠模型中显示出活性
标题:X 射线结构引导发现一种有效的口服生物可利用双人吲哚胺/色氨酸 2,3-双加氧酶 (Hido/htdo) 抑制剂,该抑制剂在帕金森病小鼠模型中显示出活性
摘要:人吲哚胺 2,3-双加氧酶 1 (Hido1) 和色氨酸 2,3-双加氧酶 (Htdo) 与帕金森病 (Pd) 的发病机制密切相关;然而,仍然缺乏开发 Hido1 和 Htdo 双重抑制剂来评估其对抗 Pd 的潜在功效.在这里,我们报告的生化,生物物理和计算分析表明,1 H-Indmaze-4-Amines 通过与血红素亚铁和三价铁态直接协调的机制抑制 Hido1 和 Htdo.晶体结构指导优化得到23,其对hido1和htdo的ic 50值分别为0.64和0.04 μm,并且在小鼠中具有非常好的药代动力学特性和脑渗透性. 23显示出对 1-甲基-4-苯基-1,2,3,6-四氢吡啶诱导的小鼠运动协调缺陷的功效,与抗 Pd 药物美多芭 (Madopar) 相当.进一步的研究表明,与madopar不同,23可能具有特定的抗pd机制,包括降低ido1表达,减轻多巴胺能神经变性,减少小鼠大脑中
DOI:10.1021/acs.Jmedchem.1C00303

专利信息

专利号:SA-109300715-B1
优先权日:2008-12-01
标 题 :Synthesis of (R)-3-((E)-2-(pyrrolidine-3-yl)-phenyl)-5-(tetrahydropyrane-4-yloxy)pyridine and forms new salts thereof

专利号:US-8633227-B2
优先权日:2008-12-01
标 题 :Synthesis and novel salt forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine
发明人：AKIREDDY SRINIVASA RAO; BREINING SCOTT R; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; GATTO GREGORY J; GENUS JOHN; HAMMOND PHILIP S; MITCHENER JR JOESPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT; YOHANNES DANIEL; FEDOROV NIKOLAI
权利人:AKIREDDY SRINIVASA RAO; BREINING SCOTT R; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; GATTO GREGORY J; GENUS JOHN; HAMMOND PHILIP S; MITCHENER JR JOESPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT; YOHANNES DANIEL; FEDOROV NIKOLAI; TARGACEPT INC
摘要:The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.

专利号:EP-1836163-B1
优先权日:2004-12-23
标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
发明人：BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
权利人:NOVARTIS AG
摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

专利号:WO-2025125811-A1
优先权日:2023-12-12
标题:Heterocyclic compounds and their use for the treatment of neurological disorders
发明人：PLOWRIGHT ALLEYN THOMAS; PFEIFFER THOMAS; MÄRCHER-RØRSTED EMIL; DUCKWORTH EDWARD JOSEPH
权利人:ONTRACK THERAPEUTICS LTD
摘要:The present invention relates to novel synthetic compounds of Formula (I) and (II) related to naturally occurring flavonoids such as 7,8-dihydroxyflavone (7,8-DHF). The invention further relates to the method of synthesis, the use of these compounds as research tools and their use as pharmaceuticals.

专利号:CA-2744197-A1
优先权日:2008-12-01
标 题 :Synthesis and novel salt forms of (r)-3-((e)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine

专利号:US-2012015983-A1
优先权日:2008-12-01
标 题 :Synthesis and Novel Salt Forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine