2-甲基-2-丙基[(3R)-1-甲基-3-吡咯烷基]氨基甲酸酯 | 346691-01-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 2-甲基-2-丙基[(3R)-1-甲基-3-吡咯烷基]氨基甲酸酯
• 英文名称: (R)-tert-butyl 1-methylpyrrolidin-3-ylcarbamate
• 英文别名: tert-butyl N-[(3R)-1-methylpyrrolidin-3-yl]carbamate
• CAS: 346691-01-8
• 化学式: C₁₀H₂₀N₂O₂
• 分子量: 200.281
• InChiKey: ZAAYKTCDODPVPD-MRVPVSSYSA-N

物化性质

• 沸点：
  280.3±29.0 °C(Predicted)
• 密度：
  1.03±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-甲基-2-丙基[(3R)-1-甲基-3-吡咯烷基]氨基甲酸酯 在 盐酸 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 (R)-1-methylpyrrolidine-3-amine hydrochloride
  参考文献：
  名称：

  Fused Ring Compound For Use As Mineralocorticoid Receptor Antagonist

  摘要：

  本发明属于医学技术领域，具体涉及以下内容：一种由化学式（I）表示的融合环化合物，用作醛固酮受体拮抗剂，其药学上可接受的盐和异构体；这些化合物的制备方法；含有这些化合物的药物制剂；以及这些化合物、其药学上可接受的盐或其异构体在制备用于治疗和/或预防肾损伤、高血压等心血管疾病和/或内分泌疾病的药物时的应用。X、Y1、Y2、Y3、R1、R2a、R2b、R3a、R3b、R4、Cy和n的定义如描述中所示。

  公开号：

  US20130289029A1
• 作为产物：
  描述：

  (3R)-(+)-1-苄基-3-(叔丁氧羰基氨基)吡咯烷 在 palladium dihydroxide sodium tetrahydroborate 、 氢气 作用下， 以 四氢呋喃 、 甲醇 、 乙醇 、 水 为溶剂， 反应 48.0h， 生成 2-甲基-2-丙基[(3R)-1-甲基-3-吡咯烷基]氨基甲酸酯
  参考文献：
  名称：

  Novel Angular Benzophenazines:  Dual Topoisomerase I and Topoisomerase II Inhibitors as Potential Anticancer Agents

  摘要：

  A series of substituted angular benzophenazines were prepared using a new synthetic route via a novel regiocontrolled condensation of 1,2-naphthoquinones and 2,3-diaminobenzoic acids. The synthesis and biological activity of this new series of substituted 8,9-benzo[a]phenazine carboxamide systems are described. The analogues were evaluated against the H69 parental human small cell lung carcinoma cell line and H69/LX4 resistant cell line which overexpresses P-glycoprotein. Selected analogues were evaluated against the COR-L23-parental human non small cell lung carcinoma cell line and the COR-L23/R resistant cell line which overexpresses multidrug resistance protein. This series of novel angular benzophenazines were potent cytotoxic agents in these cell lines and may be able to circumvent multidrug resistance mechanisms which result in the lack of efficacy of many drugs in cancer chemotherapy. These compounds show dual inhibition of topoisomerase I and topoisomerase II and thus target two key enzymes responsible for the topology of DNA that are active at different points in the cell cycle. The introduction of chirality into the carboxamide side chain of these novel benzophenazine carboxamides has resulted in the discovery of a potent enantiospecific series of cytotoxic agents, exemplified by 4-methoxy-benzo[a]phenazine-11-carboxylic acid (2-(dimethylamino)-1-(R)methyl-ethyl)-amide, XR11576 ((R)-4j"). In vivo activity has been demonstrated for 4-methoxy-benzo[a]phenazine-11-carboxylic acid (2-(dimethylamino)-1-(R)-methyl-ethyl)-amide, XR11576, after intravenous administration to female mice, and this compound has been selected as a development candidate for further evaluation.

  DOI：

  10.1021/jm010329a

文献信息

• [EN] INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE<br/>[FR] INHIBITEURS DE TYROSINE KINASE DE BRUTON ET LEURS PROCÉDÉS D'UTILISATION
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2018103058A1

  公开（公告）日：2018-06-14

  Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').

  公式（I'）的化合物及其使用和制备方法，以及包含公式（I'）化合物的组合物。
• Organic Compounds
  申请人：Maibaum Juergen Klaus

  公开号：US20090076062A1

  公开（公告）日：2009-03-19

  Disclosed are δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

  揭示了具有抑制肾素作用的δ-氨基-γ-羟基-ω-芳基-烷酸酰胺化合物的化学式(I)及其盐。还揭示了包括这些化合物的药物组合物以及用于治疗高血压、动脉粥样硬化、不稳定性冠状动脉综合征、充血性心力衰竭、心肌肥大、心脏纤维化、心肌梗死后心肌病、不稳定性冠状动脉综合征、舒张功能障碍、慢性肾病、肝纤维化、糖尿病并发症（如肾病、血管病和神经病变）、冠状血管疾病、血管成形术后再狭窄、眼内压升高、青光眼、异常血管生长、高醛固酮症、认知障碍、阿尔茨海默病、痴呆症、焦虑状态和认知障碍的治疗方法。
• [EN] PIPERIDIN-PYRIMIDINE DERIVATIVES AS ANTAGONISTS OF HISTAMINE H4 RECEPTOR<br/>[FR] DÉRIVÉS DE PIPÉRIDINE-PYRIMIDINE COMME ANTAGONISTES DES RÉCEPTEURS HISTAMINIQUES H4
  申请人：PALAU PHARMA SA

  公开号：WO2010094721A1

  公开（公告）日：2010-08-26

  Piperidin-pyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

  Piperidin-pyrimidine衍生物的化学式（I），其中不同取代基的含义如描述中所示。这些化合物可用作组胺H4受体拮抗剂。
• NOVEL COMPOUNDS
  申请人：HALSALL Christopher Thomas

  公开号：US20080009482A1

  公开（公告）日：2008-01-10

  There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.

  提供了一个化合物的化学式(I)： 其制备方法，药物组合物以及在治疗中的用途。
• Thiazole benzamide derivatives and pharmaceutical compositions for inhibiting cell proliferation, and methods for their use
  申请人：——

  公开号：US20030225147A1

  公开（公告）日：2003-12-04

  Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. 1 These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.

  氨基噻唑化合物与单取代/双取代苯甲酰胺的结构由式(I)表示，并描述了它们的药学上可接受的盐、药学上可接受的前药、药学上活性代谢物以及所述代谢物的药学上可接受的盐。 这些药物调节和/或抑制细胞增殖和蛋白激酶活性，并可用作治疗恶性肿瘤和其他疾病的药物。