tert-butyl-tetramethyl-guanidine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: tert-butyl-tetramethyl-guanidine
• 英文别名: t-butyl-tetramethylguanidine；N-t-butyl-N',N',N'',N''-tetramethylguanidine；1-tert-butyl-1,2,3,3-tetramethylguanidine
• 化学式: C₉H₂₁N₃
• 分子量: 171.286
• InChiKey: JJIXSFJJWJOGSH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  18.8
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  tert-butyl-tetramethyl-guanidine 、 (3,4-dihydronaphthalen-1(2H)-ylidene)hydrazine 在 碘 作用下， 以 乙醚 为溶剂， 反应 2.33h， 生成 1,2-二氢-4-碘萘
  参考文献：
  名称：

  [EN] 3-SUBSTITUTED-6-ARYL PYRIDINED AS LIGANDS OF C5A RECEPTORS
  [FR] 6-ARYL PYRIDINES SUBSTITUEES EN 3

  摘要：

  公开号：

  WO2004043925A3
• 作为产物：
  描述：

  叔丁胺 、 1,1,3,3-四甲基脲 在 三光气 作用下， 生成 tert-butyl-tetramethyl-guanidine
  参考文献：
  名称：

  [EN] 3-SUBSTITUTED-6-ARYL PYRIDINED AS LIGANDS OF C5A RECEPTORS
  [FR] 6-ARYL PYRIDINES SUBSTITUEES EN 3

  摘要：

  公开号：

  WO2004043925A3
• 作为试剂：
  描述：

  N-苄氧羰基甘氨酰-L-苯丙氨酸 、 L-缬氨酸甲酯盐酸盐 在 tert-butyl-tetramethyl-guanidine 、 O-(7-Azabenzotriazol-1-yl)-1,1:3,3-bis(tetramethylene)uronium hexafluorophosphate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 Cbz-Gly-D-Phe-Val-OMe 、 L,L-2-[2-(2-benzyloxycarbonylaminoacetylamino)-3-phenylpropionylamino]-3-methylbutyric acid methyl ester
  参考文献：
  名称：

  Peptide Coupling in the Presence of Highly Hindered Tertiary Amines

  摘要：

  Previously, 2,4,6-trimethylpyridine (collidine), due to steric shielding around the N-atom, was found to be an efficient base for effecting peptide segment coupling via azabenzotriazole-based onium-style coupling reagents. A number of even more highly hindered bases, including 2,3,5,6-tetramethylpyridine , 2, 6-di-tert-butyl-4-(dimethylamino)pyridine, triisopropylamine, and N-tert-butylmorpholine, have been compared with collidine in such reactions. Some of the newer bases showed advantages in terms of convenience in handling and maintenance of configuration during segment coupling processes, although dramatic differences based on steric effects were not observed. On the basis of results with a number of test peptides and many base-coupling reagent combinations, it was noted that most efficient results are obtained if 1 equiv of HOAt is present as an additive during the coupling process. For rapid activation of onium-style coupling reagents during stepwise solid-phase coupling reactions, the stronger base 2,6-di-tert-butyl-4-(dimethylamino)pyridine was more effective than collidine.

  DOI：

  10.1021/jo950912x

文献信息

• Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
  申请人：——

  公开号：US20020045747A1

  公开（公告）日：2002-04-18

  Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

  公开了抑制β-淀粉样肽释放和/或其合成的化合物，因此可用于治疗阿尔茨海默病。还公开了包含抑制β-淀粉样肽释放和/或其合成的化合物的药物组合物，以及使用这些药物组合物预防性和治疗性治疗阿尔茨海默病的方法。
• 6-O-acyl ketolide antibacterials
  申请人：——

  公开号：US20030220272A1

  公开（公告）日：2003-11-27

  6-O-Acyl ketolide antibacterials of the formula: 1 wherein R 1 , R 2 , R 3 , R 4 , W, X, X′, Y, and Y′ are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

  其中R1、R2、R3、R4、W、X、X'、Y和Y'如本文所述，并且其中取代基具有描述中指示的含义。这些化合物可用作抗菌剂。
• 3-Descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents
  申请人：——

  公开号：US20040018994A1

  公开（公告）日：2004-01-29

  3-Descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents of the formula: 1 wherein R 1 , W, R 3 , R 4 , R 5 , R 6 , X, X′, and Z are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

  3-去氧糖基-6-O-碳酰胺基和6-O-碳酸酯基大环内酯类抗菌剂，其化学公式如下： 1 其中R 1 ，W，R 3 ，R 4 ，R 5 ，R 6 ，X，X′和Z如本文及描述中所述，并且其中的取代基具有描述中指出的含义。这些化合物可用作抗菌剂。
• 11,12-Cyclic thiocarbamate macrolide antibacterial agents
  申请人：Zhu Bin

  公开号：US20050250713A1

  公开（公告）日：2005-11-10

  The present invention is directed to novel macrolide antibacterial agents and processes for preparing them. The present invention is further directed to pharmaceutical compositions containing the novel macrolide antibacterial agents disclosed herein and their use in the treatment and prevention of bacterial infections.

  本发明涉及新型大环内酯抗菌剂及其制备方法。本发明还涉及含有本文所披露的新型大环内酯抗菌剂的药物组合物，以及它们在治疗和预防细菌感染中的应用。
• [EN] PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF {1-(ETHYLSULFONYL)-3-[4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]AZETIDIN-3-YL}ACETONITRILE<br/>[FR] PROCÉDÉS ET INTERMÉDIAIRES POUR LA PRÉPARATION DE {1-(ÉTHYLSULFONYL)-3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]AZÉTIDIN-3-YL}ACÉTONITRILE
  申请人：LILLY CO ELI

  公开号：WO2016205487A1

  公开（公告）日：2016-12-22

  The present invention provides processes and intermediates for the preparation of 1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3- yl}acetonitrile: (I)

  本发明提供了制备1-(乙基磺酰基)-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]氮杂环丙烷-3-基}乙腈的过程和中间体：(I)