5-(2-(trimethylsilyloxy)-ethyl)-1,8-naphtosultam | 198472-19-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 5-(2-(trimethylsilyloxy)-ethyl)-1,8-naphtosultam
• 英文别名: 5-(2-(trimethylsilyloxy)-ethyl)-1,8-naphthosultam；2-(2,2-Dioxo-2lambda6-thia-3-azatricyclo[6.3.1.04,12]dodeca-1(11),4(12),5,7,9-pentaen-7-yl)ethoxy-trimethylsilane；2-(2,2-dioxo-2λ6-thia-3-azatricyclo[6.3.1.04,12]dodeca-1(11),4(12),5,7,9-pentaen-7-yl)ethoxy-trimethylsilane
• CAS: 198472-19-4
• 化学式: C₁₅H₁₉NO₃SSi
• 分子量: 321.472
• InChiKey: BTAWAPFOCWBJSS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.35
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  63.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N,O-双三甲硅基乙酰胺 、 5-(2-(hydroxy)-ethyl)-1,8-naphthosultam 以 四氢呋喃 、 二氯甲烷 、 苯 为溶剂， 生成 5-(2-(trimethylsilyloxy)-ethyl)-1,8-naphtosultam
  参考文献：
  名称：

  Carbapenem antibacterial compounds, compositions containing such

  摘要：

  本发明涉及一种碳青霉烯抗菌剂，其中碳青霉烯核在2位被萘磺胺基通过一个--Z--CH.sub.2基团取代。萘磺胺基进一步被各种取代基（包括阳离子基团）取代。该化合物由以下式表示：##STR1## 还包括药物组合物和使用方法。

  公开号：

  US05994343A1

文献信息

• Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
  申请人：Merck & Co., Inc.

  公开号：US06207823B1

  公开（公告）日：2001-03-27

  The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: Pharmaceutical compositions and methods of use are also included.

  本发明涉及三环头孢菌素类抗菌剂，其中头孢菌素核与一个6元碳环并联。该化合物进一步被各种取代基取代，包括至少一个阳离子基团。这些化合物由式I表示。药物组合物和使用方法也包括在内。
• Carbapenem antibacterial compounds, compositions containing such
  申请人：Merck & Co., Inc.

  公开号：US05994343A1

  公开（公告）日：1999-11-30

  The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a --Z--CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including cationic groups. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.

  本发明涉及一种碳青霉烯抗菌剂，其中碳青霉烯核在2位被萘磺胺基通过一个--Z--CH.sub.2基团取代。萘磺胺基进一步被各种取代基（包括阳离子基团）取代。该化合物由以下式表示：##STR1## 还包括药物组合物和使用方法。
• Penem antibacterial compounds, compositions and methods of treatment
  申请人：Merck & Co., Inc.

  公开号：US06271222B1

  公开（公告）日：2001-08-07

  The present invention relates to penem antibacterial agents in which the releaseable liphophilic aromatic side-chain, tethered to the carbapenem nucleus via a methylene linker, necessary for anti-MRSA activity replaces the non-releaseable liphophilic side-chains found in 2-aryl and 2-benzothiazolylthio carbapenem compounds. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: Pharmaceutical compositions and methods of use are also included.

  本发明涉及青霉烯抗菌剂，其中可释放的亲脂芳香侧链通过亚甲基连接到碳青霉烯核上，用于抗MRSA活性，取代了2-芳基和2-苯并噻唑基硫代碳青霉烯化合物中发现的不可释放的亲脂侧链。该化合物进一步被各种取代基团取代，包括至少一个阳离子基团。这些化合物由式I表示。还包括药物组合物和使用方法。
• Process for the synthesis of carbapenem intermediates, and compounds produced
  申请人：Merck & Co., Inc.

  公开号：US06489471B1

  公开（公告）日：2002-12-03

  A process of synthesizing a carbapenem compound of formula (6) is disclosed, wherein R represents H or methyl, P and P* independently represent H or protecting groups and each R1 is independently selected from: H, halo, OH, OP wherein P is a protecting group, C1-6 alkyl or C1-6 alkyl substituted with 1-3 of halo, OH, OP, NH2, NHC1-4 alkyl or N(C1-4 alkyl)2, comprising reacting a carbapenem of formula (4′) with a compound of formula (7), wherein R, R1, P and P* are as previously defined and R2 represents acetate, C(O)OR′ or P(O)(OR″)2, wherein R′ and R″ independently represent Clot alkyl, benzyl or aryl, in the presence of a catalyst to produce a compound of formula (6).

  公开了一种合成式为（6）的碳青霉烯化合物的过程，其中R代表H或甲基，P和P*分别代表H或保护基，每个R1独立选择自：H，卤，OH，OP，其中P是保护基，C1-6烷基或C1-6烷基取代1-3个卤，OH，OP，NH2，NHC1-4烷基或N（C1-4烷基）2，包括在催化剂的存在下，将式为（4'）的碳青霉烯与式为（7）的化合物反应，其中R，R1，P和P*如前所述，R2代表乙酸酯，C（O）OR'或P（O）（OR"）2，其中R'和R"独立代表Clot烷基，苄基或芳基，以产生式为（6）的化合物。
• CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
  申请人：MERCK & CO., INC.

  公开号：EP0906313B1

  公开（公告）日：2004-03-03