咪达唑仑杂质 | 119401-13-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 咪达唑仑杂质
• 英文名称: 6-chloro-4-(2-fluorophenyl)-2-methylquinazoline
• CAS: 119401-13-7
• 化学式: C₁₅H₁₀ClFN₂
• 分子量: 272.709
• InChiKey: XYJIBRYJJRDFOQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-氨基-5-氯-2'-氟二苯甲酮 、 乙腈 在 三氟甲磺酸三甲基硅酯 作用下， 以 neat (no solvent) 为溶剂， 反应 0.17h， 以75%的产率得到咪达唑仑杂质
  参考文献：
  名称：

  Lewis酸催化的腈的活化：2,4-二取代的喹唑啉和1,3-二氮杂螺[5.5]十一碳-1-烯的微波辅助无溶剂合成

  摘要：

  一种从2-氨基羰基化合物开始合成喹唑啉/喹唑啉酮和从N开始的1,3-二氮杂螺[5.5]十一碳烯-1-烯衍生物的单步，无溶剂和无过渡金属反应报道了甲苯磺酰基-2-（环己烯基）乙胺。路易斯酸催化的腈活化是该反应的关键特征。

  DOI：

  10.1002/ejoc.201701585

文献信息

• An Efficient Three-component, One-pot Synthesis of Quinazolines under Solvent-free and Catalyst-free Condition
  作者：Subrahmanya Ishwar Bhat、U. K. Das、Darshak R. Trivedi

  DOI：10.1002/jhet.2220

  日期：2015.7

  protocol for the synthesis of quinazolines in the absence of solvent and catalyst has been developed. 2,4‐Disubstituted quinazolines have been synthesized from three‐component one‐pot reactions of 2‐aminoaryl ketones, orthoesters, and ammonium acetate. The present method has advantages of operational simplicity, substrate generality, clean reaction, high yields (76–94%), and moderate reaction time. The plausible

  已经开发出在没有溶剂和催化剂的情况下合成喹唑啉的有效绿色方案。由2-氨基芳基酮，原酸酯和乙酸铵的三组分一锅法反应合成了2,4-二取代的喹唑啉。本方法具有操作简单，底物通用，反应干净，收率高（76-94％）和反应时间适中的优点。基于分离的中间体的光谱表征和单晶X射线分析，提出了反应的合理机理。
• Visible-light photocatalyzed C–N bond activation of tertiary amines: a three-component approach to synthesize quinazolines
  作者：Ajithkumar Arumugam、Gopal Chandru Senadi

  DOI：10.1039/d3ob02067c

  日期：——

  three-component approach has been developed to prepare 2,4-disubstituted quinazolines from o-acylanilines, trialkylamines and ammonium chloride under visible-light using eosin Y as the photocatalyst. The notable features of this work include (i) the use of tertiary amines as an alkyl synthon and triethanolamine as a C2-OH synthon; (ii) good functional group tolerance with 52%–98% yields; (iii) proof of

  开发了一种无金属三组分方法，以曙红 Y 作为光催化剂，在可见光下由邻酰基苯胺、三烷基胺和氯化铵制备 2,4-二取代喹唑啉。这项工作的显着特点包括（i）使用叔胺作为烷基合成子和三乙醇胺作为C 2 -OH合成子； (ii) 良好的官能团耐受性，产率 52%–98%； (iii) 以邻氨基苯甲醛为底物传递 2-甲基喹唑啉3pa的概念验证； (iv)化合物3ga 、 3ja和3ma的克级合成。基于控制研究和氧化还原电位值，提出了还原猝灭机制。
• Infusion bag of midazolam for intravenous use
  申请人：Sun Pharmaceutical Industries Limited

  公开号：US11246801B2

  公开（公告）日：2022-02-15

  The invention relates to an infusion container comprising a sterile, ready-to-use, stable aqueous solution of Midazolam or a pharmaceutically acceptable salt thereof, suitable for direct intravenous infusion to a patient in need thereof. The invention also relates to a novel infusion container having plurality of ports that is suitable for delivering or receiving a sterile fluid, such as the said stable aqueous solution of Midazolam or a pharmaceutically acceptable salt thereof.

  本发明涉及一种输液容器，内含无菌、即用、稳定的咪达唑仑水溶液或其药学上可接受的盐，适合直接静脉输注给有需要的病人。本发明还涉及一种新型输液容器，该容器具有多个端口，适用于输送或接收无菌液体，如上述稳定的咪达唑仑水溶液或其药学上可接受的盐。
• INFUSION BAG OF MIDAZOLAM FOR INTRAVENOUS USE
  申请人：Sun Pharmaceutical Industries Limited

  公开号：US20200268606A1

  公开（公告）日：2020-08-27

  The invention relates to an infusion container comprising a sterile, ready-to-use, stable aqueous solution of Midazolam or a pharmaceutically acceptable salt thereof, suitable for direct intravenous infusion to a patient in need thereof. The invention also relates to a novel infusion container having plurality of ports that is suitable for delivering or receiving a sterile fluid, such as the said stable aqueous solution of Midazolam or a pharmaceutically acceptable salt thereof