1-[[7-(3,4-Dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5-a]pyrimidin-6-yl]carbonyl]-L-proline methyl ester | 343243-12-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 1-[[7-(3,4-Dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5-a]pyrimidin-6-yl]carbonyl]-L-proline methyl ester
• 英文别名: methyl (2S)-1-[7-(3,4-dichlorophenyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidine-6-carbonyl]pyrrolidine-2-carboxylate
• CAS: 343243-12-9
• 化学式: C₂₀H₂₀Cl₂N₄O₃
• 分子量: 435.31
• InChiKey: ADLUNWXXEBRVEK-BUSXIPJBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  76.5
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  7-(3,4-Dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5-a]pyrimidine-6-carboxylic acid 、 L-脯氨酸甲酯 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 生成 1-[[7-(3,4-Dichlorophenyl)-4,7-dihydro-5-methylpyrazolo[1,5-a]pyrimidin-6-yl]carbonyl]-L-proline methyl ester
  参考文献：
  名称：

  Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers

  摘要：

  Design and synthesis of pyrazolodihydropyrimidines as K(V)1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed atrial selective prolongation of effective refractory period in rabbits and was selected for clinical development. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.12.085

文献信息

• Heterocyclic dihydropyrimidine compounds
  申请人：——

  公开号：US20030022890A1

  公开（公告）日：2003-01-30

  Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the K v 1 subfamily of voltage gated K + channels, especially inhibitors K v 1.5 which has been linked to the ultra-rapidly activating delayed rectifier K + current I Kur ), methods of using such compounds in the prevention and treatment of arrhythmia and I Kur -associated conditions, and pharmaceutical compositions containing such compounds.

  本发明涉及一种新型杂环二氢嘧啶化合物，其可作为钾通道功能抑制剂（特别是Kv1亚家族电压门控K+通道的抑制剂，特别是与超快速激活延迟整流K+电流IKur相关的Kv1.5的抑制剂），以及使用这些化合物在预防和治疗心律失常和IKur相关疾病方面的方法，以及含有这些化合物的药物组合物。
• [EN] HETEROCYCLIC DIHYDROPYRIMIDINES AS POTASSIUM CHANNEL INHIBITORS<br/>[FR] DIHYDROPYRIMIDINES HETEROCYCLIQUES UTILES EN TANT QU'INHIBITEURS DES CANAUX POTASSIUM
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2001040231A1

  公开（公告）日：2001-06-07

  Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors K¿v?1.5 which has been linked to the ultra-rapidly activating delayed rectifier K?+¿ current I¿Kur?), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

  新型杂环二氢嘧啶化合物可作为钾通道功能抑制剂使用（特别是Kv1亚家族电压门控K+通道的抑制剂，特别是与超快速激活延迟整流K+电流IKur相关的Kv1.5抑制剂），使用这种化合物预防和治疗心律失常和IKur相关疾病的方法，以及含有这种化合物的制药组合物。
• HETEROCYCLIC DIHYDROPYRIMIDINES AS POTASSIUM CHANNEL INHIBITORS
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：EP1237891A1

  公开（公告）日：2002-09-11
• US7157451B2
  申请人：——

  公开号：US7157451B2

  公开（公告）日：2007-01-02
• US7541362B2
  申请人：——

  公开号：US7541362B2

  公开（公告）日：2009-06-02