2-(trimethylstannyl)-5-chloropyridine | 198985-47-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-(trimethylstannyl)-5-chloropyridine
• 英文别名: 5-chloro-2-(trimethylstannyl)pyridine；5-chloro-2-trimethylstannanylpyridine；2-trimethylstannanyl-5-chloropyridine；(5-chloropyridin-2-yl)-trimethylstannane
• CAS: 198985-47-6
• 化学式: C₈H₁₂ClNSn
• 分子量: 276.353
• InChiKey: MOXPZHRWZDWGLZ-UHFFFAOYSA-N

物化性质

• 沸点：
  243.3±50.0 °C(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.28
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  ethyl 5-bromo-1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylate 、 2-(trimethylstannyl)-5-chloropyridine 在 四(三苯基膦)钯 作用下， 以 1,4-二氧六环 为溶剂， 反应 1.0h， 生成 Ethyl 5-(5-chloropyridin-2-yl)-1-[(4-methoxyphenyl)methyl]triazole-4-carboxylate
  参考文献：
  名称：

  [EN] GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
  [FR] INHIBITEURS DE GLYCOLATE OXYDASE POUR LE TRAITEMENT D'UNE MALADIE

  摘要：

  本文描述了化合物、制备这种化合物的方法、含有这种化合物的药物组合物和药物，以及使用这种化合物治疗或预防与甘氧酸代谢缺陷相关的疾病或紊乱的方法，例如与甘氧酸氧化酶（GO）或草酸代谢变化相关的疾病或紊乱。这些疾病或紊乱包括与产生过多草酸相关的甘氧酸代谢紊乱，例如原发性高草酸尿症。

  公开号：

  WO2020257487A1
• 作为产物：
  描述：

  (5-氯吡啶-3-基)三氟甲磺酸酯 在 Pd(PPh3)4 2,6-二叔丁基-4-甲基苯酚 、 六甲基二锡 、 lithium chloride 作用下， 以 甲苯 为溶剂， 生成 2-(trimethylstannyl)-5-chloropyridine
  参考文献：
  名称：

  Pyridinyl-2-cyclopenten-1-ones as selective cyclooxygenase-2 inhibitors

  摘要：

  这项发明涵盖了式I的新化合物，以及治疗COX-2介导疾病的方法，包括向需要此类治疗的患者施用式I化合物的非毒性治疗有效量。 该发明还涵盖了用于治疗COX-2介导疾病的某些药物组合物，其中包括式I的化合物。

  公开号：

  US05922742A1

文献信息

• Pyridyl inhibitors of hedgehog signalling
  申请人：Gunzner L. Janet

  公开号：US20060063779A1

  公开（公告）日：2006-03-23

  The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R 1 , R 2 , R 3 , R 4 , m and n are as described herein.

  这项发明提供了一种新型的刺刺信号抑制剂，可用作治疗恶性肿瘤的治疗剂，其中化合物具有一般式I： 其中A、X、Y、R1、R2、R3、R4、m和n如本文所述。
• HETEROCYCLIC COMPOUND
  申请人：Sumitomo Chemical Company, Limited

  公开号：US20190127328A1

  公开（公告）日：2019-05-02

  A compound of formula (I), or an N-oxide thereof is provided. In the compound of formula (I), Het 1 represents Het 1 -1, Het 1 -2, Het 1 -3, Het 1 -4, Het 1 -5, Het 1 -6, Het 1 -7, Het 1 -8, or Het 1 -9, and the remaining variable groups are as defined in the specification. The compound of formula (I), or N-oxide thereof has a superior effect in controlling arthropod pests.

  提供了一种具有式（I）的化合物，或其N-氧化物。在式（I）的化合物中，Het1代表Het1-1、Het1-2、Het1-3、Het1-4、Het1-5、Het1-6、Het1-7、Het1-8或Het1-9，其余的变量基团如规范中所定义。式（I）的化合物或其N-氧化物在控制节肢动物害虫方面具有卓越效果。
• PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING
  申请人：Gunzner Janet L.

  公开号：US20090281089A1

  公开（公告）日：2009-11-12

  The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R 1 , R 2 , R 3 , R 4 , m and n are as described herein.

  本发明提供了一种新型的刺猬信号抑制剂，其可用作治疗恶性肿瘤的治疗剂，其中化合物具有一般式I，其中A、X、Y、R1、R2、R3、R4、m和n如本文所述。
• 2,3-Diarylcyclopentenones as Orally Active, Highly Selective Cyclooxygenase-2 Inhibitors
  作者：W. Cameron Black、Christine Brideau、Chi-Chung Chan、Stella Charleson、Nathalie Chauret、David Claveau、Diane Ethier、Robert Gordon、Gillian Greig、Jocelyne Guay、Gregory Hughes、Paule Jolicoeur、Yves Leblanc、Deborah Nicoll-Griffith、Nathalie Ouimet、Denis Riendeau、Denise Visco、Zhaoyin Wang、Lijing Xu、Petpiboon Prasit

  DOI：10.1021/jm980642l

  日期：1999.4.1

  Cyclopentenones containing a 4-(methylsulfonyl)phenyl group in the 3-position and a phenyl ring in the 2-position are selective inhibitors of cyclooxygenase-2 (COX-2). The selectivity for COX-2 over COX-1 is dramatically improved by substituting the 2-phenyl group with halogens in the meta position or by replacing the phenyl ring with a 2- or 3-pyridyl ring. Thus the 3,5-difluorophenyl derivative 7 (L1776,967) and the 3-pyridyl derivative 13 (L-784,506) are particularly interesting as potential antiinflammatory agents with reduced side-effect profiles. Both exhibit good oral bioavailability and are potent in standard models of pain, fever, and inflammation yet have a much reduced effect on the GI integrity of rats compared to standard nonsteroidal antiflammatory drugs.
• Discovery of (1<i>S</i>,2<i>R</i>,3<i>R</i>)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors
  作者：Makoto Shiozaki、Katsuya Maeda、Tomoya Miura、Masayuki Kotoku、Takayuki Yamasaki、Isamu Matsuda、Kenta Aoki、Katsutaka Yasue、Hiroto Imai、Minoru Ubukata、Akira Suma、Masahiro Yokota、Takahiro Hotta、Masahiro Tanaka、Yasunori Hase、Julia Haas、Andrew M. Fryer、Ellen R. Laird、Nicole M. Littmann、Steven W. Andrews、John A. Josey、Takayuki Mimura、Yuichi Shinozaki、Hiromi Yoshiuchi、Takashi Inaba

  DOI：10.1021/jm101609j

  日期：2011.4.28

  Aggrecanases, particularly aggrecanase-1 (ADAMTS-4) and aggrecanase-2 (ADAMTS-5), are believed to be key enzymes involved in the articular cartilage breakdown that leads to osteoarthritis. Thus, aggrecanases are considered to be viable drug targets for the treatment of this debilitating disease. A cries of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates was discovered to be potent, highly selective, aid orally bioavailable aggrecanase inhibitors. These compounds have unique P1' groups comprising novel piperidine- or piperazin e-based heterocycles that are connected to a cyclopropane amino acid scaffold via a sulfamido linkage. These P1' groups are quite effective in imparting selectivity over other MMPs, and this selectivity was further increased by incorporation of a methyl substituent in the 2-position of the cyclopropane ring. In contrast to classical hydroxamate-based inhibitors that tend to lack metabolic stability, our aggrecanase inhibitors bear a carboxylate zinc-binding group and have good oral bioavailability. Lead compound 13b, characterized by the novel P1' portion of 1,2,3,4-tetrahydropyrido[3',4':4,5]imidazo [1,2-a]-pyridine ring, is a potent and selective aggrecanse inhibitor with excellent pharmacokinetic profiles.