CAS: 202197-26-0; 3-Chloro-4-((3-Fluorobenzyl)Oxy)Aniline

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CAS号443882-99-3 3-氯-4-(3-氟苄氧基)硝基苯 | CAS号878018-19-0 2-chloro-1-(3-f... | CAS号619-08-9 2-氯-4-硝基酚 | CAS号456-41-7 3-氟苄溴 | CAS号350-30-1 3-氯-4-氟硝基苯 | CAS号456-47-3 3-氟苄醇 | CAS号388082-78-8 二甲苯磺酸拉帕替尼 | CAS号897383-62-9 N-[4-[[3-氯-4-[(... | CAS号1050500-29-2 艾力替尼 | CAS号231278-84-5 5-[4-[[3-氯-4-[(... | CAS号231278-20-9 N-[3-氯-4-(3-氟苄氧... | CAS号231277-92-2 拉帕替尼 | CAS号848133-17-5 HKI-357 | CAS号388082-81-3 GW 583340二盐酸盐

2-氯-4-硝基苯酚置于铁粉,Potassium Carbonate,氯化铵体系中,用 乙醇,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 1.12H,反应生成3-氯-4-(3-氟苄氧基)苯胺
参考文献:发现新型有效的基于 Safinamide 的衍生物作为治疗帕金森病 (Pd) 的高选择性 Hmao-B 抑制剂:设计,合成,体外,体内和计算机生物学研究
标题:发现新型有效的基于 Safinamide 的衍生物作为治疗帕金森病 (Pd) 的高选择性 Hmao-B 抑制剂:设计,合成,体外,体内和计算机生物学研究
摘要:迄今为止,目前的临床实践仅采用对症治疗来管理帕金森病(pd),但无法阻止疾病进展.发现具有强效和选择性人单胺氧化酶 B ( H Mao-B) 抑制活性的新化学实体是临床相关主题.在此,Safinamide(一种众所周知的第二代h Mao-B 抑制剂)的结构优化策略提供了一系列 36 种 Safinamide 衍生的新类似物(4Aa-Bj).大多数化合物显示有希望的对抗抑制活性ħ Mao-B(> 70%抑制在10μm的单一剂量浓度),与上没有明显效果ħ100 μm 的 Mao-A.此外,虽然六种化合物(4Ak,4As,4Az,4Be,4Bg和4Bi)在h Mao-B 上表现出有效的两位数纳摩尔活性,Ic 50值为29.5,42.2,22.3,18.8,42.2和33M.分别具有相同羧酰胺部分(2-吡嗪基)的三种衍生物(4Aq,4At和4Bf)显示出最有效的单位数纳摩尔活性(ic 50分别为9
Doi:10.1016/j.Bioorg.2021.105233

专利信息

专利号:US-9359333-B2
优先权日:2013-01-14
标 题 :Efficient process for the preparation of Lapatinib and salts thereof by means of new intermediates
发明人：FONTANA FRANCESCO; PAIO ALFREDO
权利人:F I S —FABBRICA ITALIANA SINT S P A; F I S —FABBRICA ITALIANA SINT
摘要:The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. n In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.

专利号:US-8853396-B2
优先权日:2011-03-25
标 题:Methods for the preparation of lapatinib and the salts thereof
发明人：FONTANA FRANCESCO
权利人:FONTANA FRANCESCO; ITALIANA SINT SPA
摘要:Methods for the synthesis of the pharmaceutically active ingredient Lapatinib and the salts thereof are provided. In particular, such methods utilize intermediates in which the hydroxyl function is protected by a tetrahydropyranyl group providing greater solubility of the intermediates in common organic solvents.

专利号:WO-2013080218-A1
优先权日:2011-11-28
标 题 :Novel intermediates and process for the preparation of lapatinib and its pharmaceutically acceptable salts
发明人：LAHIRI SASWATA; GUPTA NITIN; SINGH HEMANT KUMAR; HANDA VISHAL; SANGHANI SUNIL
权利人:FRESENIUS KABI ONCOLOGY LTD
摘要:The present invention discloses novel intermediates and processes for the synthesis of Lapatinib and its pharmaceutically acceptable salts thereof.

专利号:WO-2014170910-A1
优先权日:2013-04-04
标 题:Process for the preparation of lapatinib
发明人：MUDDASANI PULLA REDDY; TALASILA SAMBASIVA RAO; SATTI VENKATA REDDY; NEKKANTI SATISH CHOWDARY; NANNAPANENI VENKAIAH CHOWDARY
权利人:NATCO PHARMA LTD
摘要:Present process relates to an improved and commercial process for the preparation of lapatinib of formula-I or its pharmaceutically acceptable p-toluenesulfonate salt involving novel intermediates of formulae-XVII, XVIII, and XIX. Present process utilizes Meerwein reaction as a key step in the aryl C-C bond formation step avoiding costly boronate coupling chemistry used in the conventional synthesis of lapatinib.

专利号:WO-2023098592-A1
优先权日:2021-11-30
标题:Preparation method for carbon-loaded iron-based catalyst and use thereof in synthesis of intermediates of anti-cancer inhibitors

专利号:CN-108484541-B
优先权日:2018-04-11
标 题 :Synthesis method of 5-formyl furan-2-ethyl nitrobenzoate