CAS: 521284-21-9; (R)-2-[[2-(4-Nitrophenyl)Ethyl]Amino]-1-Phenylethanol Hydrochloride

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CAS号521284-22-0 (alphaR)-alpha-...

D-扁桃酸置于sodium Tetrahydroborate,硼酸三甲酯,三氟化硼乙醚,N,N-二异丙基乙胺体系中,用 四氢呋喃,乙腈 作为反应溶剂,化学反应 23.0H,反应生成 (Alphar)-Alpha-[[[2-(4-硝基苯基)乙基]氨基]甲基]苯甲醇盐酸盐
参考文献:发现用于细胞成像和 Nanobret 检测的 β-肾上腺素能受体的环境敏感荧光配体
标题:发现用于细胞成像和 Nanobret 检测的 β-肾上腺素能受体的环境敏感荧光配体
摘要:通过将几种对环境敏感的荧光团与药效团米拉贝隆融合,产生了一系列新的β-肾上腺素能受体(β-Ars)荧光配体,具有开启机制和对β-Ars的高结合亲和力.经系统比较和优化后,具有吡啶鎓部分的化合物l5具有最佳的综合性能,包括高亲和力和可接受的细胞毒性,与β-Ars结合后显着的荧光增强(高达30倍),以及β-Ars的可视化能力.免洗条件下活细胞中的 Ar.此外,基于化合物l5的基于 Nanoluc 的生物发光共振能量转移 (Nanobret) 结合测定由于其独特的荧光光谱特征,已开发并可能用于β-Ars药物发现的高通量筛选(hts).总体而言,作为第一个对环境敏感的荧光配体,分子l5可能是了解 β-Ars 药理学的有用工具.
DOI:10.1021/acs.Analchem.1C05646

专利信息

专利号:US-9815771-B2
优先权日:2014-08-06
标题 :Method for the synthesis of mirabegron and its derivatives
发明人：MARQUILLAS OLONDRIZ FRANCISCO; RIEGO ARBOLEYA ESTELA
权利人:INTERQUIM SA
摘要:The present invention refers to a method for the synthesis of a compound of formula (I), solvates, stereoisomers or salts thereof, a key intermediate in the synthesis of Mirabegron by reduction of an amide in the presence of an amine-boranecomplex, wherein the amine is an aniline.

专利号:EP-3177589-A1
优先权日:2014-08-06
标题 :Method for the synthesis of mirabegron and its derivatives

专利号:US-7982049-B2
优先权日:2001-10-30
标 题:α-form or β-form crystal of acetanilide derivative
发明人：KAWAZOE SOUICHIROU; SAKAMOTO KENICHIROU; AWAMURA YUJI; MARUYAMA TATSUYA; SUZUKI TAKAYUKI; ONDA KENICHI; TAKASU TOSHIYUKI
权利人:ASTELLAS PHARMA INC
摘要:To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.

专利号:EP-3177589-B1
优先权日:2014-08-06
标题:Method for the synthesis of mirabegron and its derivatives

专利号:CN-108658797-A
优先权日:2018-06-19
标题 :Synthesis of a mirabegron intermediate (R)-2-(4-nitrophenethylamino)-1-phenylethanol hydrochloride

专利号:WO-2016020440-A1
优先权日:2014-08-06
标题 :Method for the synthesis of mirabegron and its derivatives