5-(4-(tert-butyl)phenyl)-4-methylthiazole

• 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: 5-(4-(tert-butyl)phenyl)-4-methylthiazole
• 英文别名: 5-(4-Tert-butylphenyl)-4-methyl-1,3-thiazole；5-(4-tert-butylphenyl)-4-methyl-1,3-thiazole
• 化学式: C₁₄H₁₇NS
• 分子量: 231.362
• InChiKey: SVXWLZQWOBEYPC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  4-甲基噻唑 、 1-叔丁基-3-碘苯 在 Pd(opiv)2 、 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 以60%的产率得到5-(4-(tert-butyl)phenyl)-4-methylthiazole
  参考文献：
  名称：

  Reigoselective Arylation of Thiazole Derivatives at 5-Position via Pd Catalysis under Ligand-Free Conditions

  摘要：

  An efficient regioselective arylation of thiazole derivatives via Pd-catalyzed C-H activation is reported. The transformation was hypothesized through a Pd(0/II) catalytic cycle in the absence of special ligand sets. This method provided an efficient process to direct arylation of thiazoles at the 5-position.

  DOI：

  10.1021/ol4027073

文献信息

• MASP-2 INHIBITORS AND METHODS OF USE
  申请人：Omeros Corporation

  公开号：US20210171461A1

  公开（公告）日：2021-06-10

  The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.

  本公开提供了具有MASP-2抑制活性的化合物，这些化合物的组合物，以及制备和使用这些化合物的方法。
• Methods of Inhibiting MASP-2 for the Treatment and/or Prevention of Coronavirus-induced Acute Respiratory Distress Syndrome
  申请人：Omeros Corporation

  公开号：US20210292436A1

  公开（公告）日：2021-09-23

  In one aspect, the invention provides methods for treating, inhibiting, alleviating, or preventing acute respiratory distress syndrome, pneumonia, or some other pulmonary or other manifestation of coronavirus infection, such as thrombosis, in a mammalian subject infected with coronavirus, such as SARS-CoV-2. The methods comprise the step of administering to a subject infected with coronavirus an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In one embodiment, the MASP-2 inhibitory agent is a MASP-2 monoclonal antibody, or fragment thereof that specifically binds to a portion of SEQ ID NO:6. In one embodiment, the MASP-2 inhibitory agent is a small molecule MASP-2 inhibitory compound. In one embodiment, the subject is a human subject suffering from COVID-19-induced acute respiratory distress syndrome (ARDS) and requires supplemental oxygen prior to treatment and the MASP-2 inhibitory agent is administered in an amount sufficient to discontinue the need for supplemental oxygen.
• BIOMARKER FOR ASSESSING THE RISK OF DEVELOPING ACUTE COVID-19 AND POST-ACUTE COVID-19
  申请人：Omeros Corporation

  公开号：US20220308056A1

  公开（公告）日：2022-09-29

  Disclosed herein are compositions, kits and methods for determining the concentration of fluid-phase MASP-2/C1-INH complex in a biological fluid, such as a biological fluid obtained from a subject infected with SARS-CoV-2. Also disclosed are methods of using said compositions, methods and kits for detection of MASP-2/C1-INH complex to determine the status of lectin pathway activation in a mammalian subject and thereby assess the risk of a subject that is or has been infected with SARS-CoV-2 for developing COVID-19-related ARDS or other poor outcome, or determine the need for treatment or efficacy of treatment of a subject in need thereof with a complement inhibitor such as a MASP-2 inhibitory agent.