2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[2-(2-hydroxyphenyl)ethylamino]ethyl]phenyl]acetamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[2-(2-hydroxyphenyl)ethylamino]ethyl]phenyl]acetamide
• 化学式: C₂₁H₂₄N₄O₂S
• 分子量: 396.5
• InChiKey: GLRIEFIBWXIZES-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  28
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  129
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF 2-(2-AMINOTHIAZOL-4-YL)-N-[4-(2-[[(2R)-2-HYDROXY-2- PHENYLETHYL]AMINO]-ETHYL)PHENYL]ACETAMIDE<br/>[FR] PROCÉDÉ AMÉLIORÉ DE PRÉPARATION DE 2-(2-AMINOTHIAZOL-4-YL)-N-[4-(2-[[(2R)-2-HYDROXY-2-PHÉNYLÉTHYL] AMINO]-ÉTHYL)PHÉNYL]ACÉTAMIDE
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2015155664A1

  公开（公告）日：2015-10-15

  The present invention relates to an improved process for the preparation of pure 2-(2- amino-1,3-thiazol-4-yl)-N-[4-(2-[(2R)-2-hydroxy-2-phenylethyl]amino]ethylphenyl]- acetamide of formula (1) substantially free of impurities. The present invention relates to the novel process of preparing intermediate (R)-1- Phenyl-2-[[2-(4-nitrophenyl)ethyl]amino]ethanol hydrochloride of formula (2) in high yield, which is useful in the preparation of mirabegron of formula (1). The process also relates to the preparation of pure α –form crystal of 2-(2-Amino- 1,3-thiazol-4-yl)-N-[4-(2-[(2R)-2-hydroxy-2-phenylethyl]amino]ethylphenyl]acetamide Mirabegron (1) without isolation of β-form.

  本发明涉及一种改进的工艺，用于制备纯度高的2-(2-氨基-1,3-噻唑-4-基)-N-[4-(2-[(2R)-2-羟基-2-苯乙基]氨基)乙基苯基]-乙酰胺，其化学式为(1)，基本上不含杂质。本发明涉及一种新的工艺，用于高产率制备中间体(R)-1-苯基-2-[[2-(4-硝基苯基)乙基]氨基]乙醇盐酸盐，其化学式为(2)，该中间体在制备化合物mirabegron的过程中很有用。该工艺还涉及制备纯度高的α-型晶体的2-(2-氨基-1,3-噻唑-4-基)-N-[4-(2-[(2R)-2-羟基-2-苯乙基]氨基)乙基苯基]乙酰胺mirabegron(1)，而无需分离β-型晶体。
• [EN] PROCESS FOR THE PREPARATION OF 2-(2-AMINOTHIAZOL-4-YL)-N-[4-(2-{[(2R)-2-HYDROXY-2-PHENYL ETHYL]AMINO}ETHYL)PHENYL]ACETAMIDE MONOHYDROCHLORIDE, ITS INTERMEDIATES AND POLYMORPH THEREOF<br/>[FR] PROCÉDÉ DE PRÉPARATION DE MONOCHLORYDRATE D'ACÉTAMIDE 2- (2-AMINOTHIAZOL -4-YL)-N- [4- (2- {[ (2R) -2-HYDROXY -2-PHÉNYL-ÉTHYL] AMINO} ÉTHYL) PHÉNYL], DE SES INTERMÉDIAIRES ET POLYMORPHE DE CELUI-CI
  申请人：MSN LAB LTD

  公开号：WO2014132270A2

  公开（公告）日：2014-09-04

  The present invention relates to a process for the preparation of 2-(2-aminothiazol-4-yl)- N-[4-(2- [(2R)-2-hydroxy-2-phenylethyl]amino} ethyl)phenyl]acetamide monohydrochloride compound of formula- la, its intermediates and polymorph thereof. [Formula should be inserted here]

  本发明涉及一种制备2-(2-氨基噻唑-4-基)-N-[4-(2-[(2R)-2-羟基-2-苯乙基]氨基}乙基)苯基]乙酰胺单盐酸盐化合物的方法，其中间体和多晶形式。[公式应在此处插入]
• DOSING REGIMENS FOR BETA-3 ADRENOCEPTOR AGONISTS AND ANTI-MUSCARINIC AGENTS FOR THE TREATMENT AND PREVENTION OF LOWER URINARY TRACT SYMPTOMS AND OVERACTIVE BLADDER
  申请人：Velicept Therapeutics, Inc.

  公开号：EP3463312A1

  公开（公告）日：2019-04-10
• US9815771B2
  申请人：——

  公开号：US9815771B2

  公开（公告）日：2017-11-14
• [EN] DOSING REGIMENS FOR BETA-3 ADRENOCEPTOR AGONISTS AND ANTI-MUSCARINIC AGENTS FOR THE TREATMENT AND PREVENTION OF LOWER URINARY TRACT SYMPTOMS AND OVERACTIVE BLADDER<br/>[FR] SCHÉMAS POSOLOGIQUE POUR AGONISTES DE RÉCEPTEURS ADRÉNERGIQUES BÊTA-3 ET AGENTS ANTI-MUSCARINIQUES POUR LE TRAITEMENT ET LA PRÉVENTION DE SYMPTÔMES DU BAS APPAREIL URINAIRE ET D'UNE HYPERACTIVITÉ VÉSICALE
  申请人：VELICEPT THERAPEUTICS INC

  公开号：WO2017210696A1

  公开（公告）日：2017-12-07

  Embodiments relate to pharmaceutical compositions, comprising one or more beta-3 adrenoceptor agonists that are useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder, prostate disorders and methods for treating lower urinary tract symptoms utilizing the pharmaceutical compositions, comprising one or more beta-3 adrenoceptor agonists. In some embodiments, the pharmaceutical compositions, comprising one or more beta-3 adrenoceptor agonists comprise pulsatile drug delivery systems. Embodiments further relate to a dosing regimen, comprising beta-3 adrenoceptor agonists and anti-muscarinic agents that are both useful for the treatment of lower urinary tract symptoms; methods for treating lower urinary tract symptoms methods utilizing the dosing regimens, comprising beta-3 adrenoceptor agonists anti-muscarinic agents; and consumer packaging, comprising both beta-3 adrenoceptor agonists and anti-muscarinic agents packaged and arranged to ensure patient compliance.