CAS: 391901-45-4; Mirabegron Impurity-1

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p-Aminophenethylamine (R)-Styrene oxide (S)-styrene oxide (R)-2-[[2′-(4-nitrophenyl)ethyl]amino]-1-phenylethanol hydr°Chloridetert-butyl 4-[(2,4-dioxo-1,3-thiazolidin-5-yl)amino]phenethyl[(2 R)-2-hydroxy-2-phenylethyl]carbamate (R)-2-(2-aminothiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide (R)-(4-aminophenylethyl)(2-hydroxy-2-phenylethyl)carbamic acid tert-butyl ester

📜米拉贝隆置于cholinesterase体系中,化学反应生成 米拉贝隆杂质
参考文献:Identification Of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible For The Glucuronidation Of Mirabegron,A Potent And Selective β3-Adrenoceptor Agonist,In Human Liver Microsomes
标题:Identification Of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible For The Glucuronidation Of Mirabegron,A Potent And Selective β3-Adrenoceptor Agonist,In Human Liver Microsomes
摘要:米拉贝隆通过多种机制清除,包括药物代谢酶.最主要的清除途径之一是直接葡糖醛酸化.在人类中,已鉴定出m11(o-葡糖苷酸),M13(氨基甲酰-葡糖苷酸)和m14(n-葡糖苷酸),其中m11是人类血浆中的主要代谢物之一.本研究旨在使用人肝微粒体(hlm)和重组人ugts(rhugts)识别负责米拉贝隆直接葡糖醛酸化的尿苷5'-二磷酸(udp)-葡糖醛酸基转移酶(ugt)同工酶.反应混合物包含1-1000 μm的米拉贝隆,8 Mm Mgcl2,白粉菌素(25 μg/ml),50 Mm Tris-Hcl缓冲液(ph 7.5),人肝微粒体(hlm)或rhugt(1.0 Mg蛋白/ml),以及2 Mm Udp-葡萄糖醛酸,总体积为200 μl,在37 oc下反应120分钟.从16个人中使用的hlms进行了相关性研究,并使用甲芬那酸和丙泊酚进行了抑制研究.关于m11形成,在测试的rhugt中,Rhugt2B7表现出高活性(11.3 Pmol/min/mg蛋白).这个结果得到了个体hlm中m11形成活性和ugt2B7标记酶活性(吗啡的3-葡糖醛酸化,R 2 = 0.330,P = 0.020)之间的相关性;池化hlms中甲芬那酸的抑制作用(ic50 = 22.8 μm);以及池化hlms和rhugt2B7之间的相对相似的k M值(1260 Vs. 486 μm)的支持.关于m13和m14形成,在测试的rhugt中,Rhugt1A3和rhugt1A8分别表现出高活性.ugt2B7是hlms中m11形成的主要催化剂.关于m13和m14形成,Ugt1A3和ugt1A8分别是葡糖醛酸化的强有力候选者.
DOI:10.1007/s13318-017-0450-X

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: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:US-2017226045-A1
优先权日:2014-08-06
标 题:Method for the synthesis of mirabegron and its derivatives

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:ES-2676586-T3
优先权日:2014-08-06
标题 :Procedure for the synthesis of mirabegron and its derivatives

专利号:CN-110862359-B
优先权日:2019-11-19
标 题:Synthesis method of mirabegron