4-(tributylstannyl)-N-Boc-aniline | 185399-96-6

• 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: 4-(tributylstannyl)-N-Boc-aniline
• 英文别名: N-(t-butoxycarbonyl)-4-tributylstannylaniline；(4-tributylstannanyl-phenyl)-carbamic acid tert-butyl ester；tert-butyl N-(4-tributylstannylphenyl)carbamate
• CAS: 185399-96-6
• 化学式: C₂₃H₄₁NO₂Sn
• 分子量: 482.294
• InChiKey: SSAUPJVGRJWUPW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.09
• 重原子数：
  27
• 可旋转键数：
  13
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(tributylstannyl)-N-Boc-aniline 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 生成 p-H2NC6H4Snn-Bu3
  参考文献：
  名称：

  用于诊断或治疗表达前列腺特异性膜抗原肿瘤的新型核素标记巯基衍生物及其应用

  摘要：

  本申请提供用于诊断或治疗表达前列腺特异性膜抗原的癌症的标记抑制剂，所述抑制剂为通式Ⅰ所示化合物#imgabs0#或通式II所示化合物#imgabs1#或通式III所示化合物#imgabs2#或其旋光异构体、药学上可接受的盐和/或溶剂化物，本申请还提供它们的制备方法以及含有所述化合物的药物组合物。本发明还涉及该类化合物及其药学上可接受的盐、溶剂化物或其前药在治疗中作为治疗表达PSMA癌症的用途。

  公开号：

  CN117430537A
• 作为产物：
  描述：

  二碳酸二叔丁酯 、 4-溴苯胺 在 三苯基膦钯 sodium hexamethyldisilazane 、 三乙胺 作用下， 以 四氢呋喃 、 乙酸乙酯 、 甲苯 为溶剂， 生成 4-(tributylstannyl)-N-Boc-aniline
  参考文献：
  名称：

  Sulfonamide derivatives

  摘要：

  本发明提供了某些磺胺类衍生物，可用于增强哺乳动物的谷氨酸受体功能，因此，可用于治疗各种疾病，如精神疾病和神经系统疾病。

  公开号：

  US06500865B1

文献信息

• Sulphonamide derivatives
  申请人：Eli Lilly and Company

  公开号：US06303816B1

  公开（公告）日：2001-10-16

  Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R1—L—NHSO2R2  I in which R1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.

  在哺乳动物中，使用有效量的公式 I 所示化合物的谷氨酸受体功能可以被增强：R1—L—NHSO2R2  I 其中：R1 代表未取代或取代的芳香族或杂芳族基团；R2 代表 (1-6C) 烷基，(3-6C) 环烷基，(1-6C) 氟代烷基，(1-6C) 氯代烷基，(2-6C) 烯丙基，(1-4C) 烷氧基(1-4C) 烷基，未取代或被卤素、(1-4C) 烷基或(1-4C) 烷氧基取代的苯基，或者一个由 R3R4N 组成的基团，其中 R3 和 R4 各自独立地代表 (1-4C) 烷基，或者与它们所连接的氮原子一起形成一个氮杂环丁烷基、吡咯烷基、哌啶基、吗啡啉基、哌嗪基、六氢氮杂环庚基或八氢氮杂环辛基；L 代表一个未取代或取代有一个或两个独立选择的(1-6C) 烷基、芳基(1-6C) 烷基、(2-6C) 烯丙基、芳基(2-6C) 烯丙基和芳基的 (2-4C) 烷烯链，或者两个取代基，它们与它们所连接的碳原子或碳原子一起形成一个 (3-8C) 碳环烷基；以及它们的药物可接受的盐。还公开了公式 I 的化合物、它们的制备过程以及包含它们的药物组合物。
• Synthesis of an esperamicin core analog with an epoxide trigger
  作者：Harold Mastalerz、Terrence W Doyle、John F Kadow、Dolatrai M Vyas

  DOI：10.1016/s0040-4039(96)02009-6

  日期：1996.11

  An esperamicin core analog 4 with an epoxide trigger like that found in the related enediyne, dynemicin, was prepared. Surprisingly, it was found to be relatively stable; the p-aminophenyl substituent did not facilitate epoxide solvolysis to the extent that had been anticipated. A mild acid, pyridinium p-toluenesulfonate, was found to induce solvolysis of 4 and led to the formation of the cycloaromatized

  制备了具有环氧化物引发剂的埃斯帕米霉素核心类似物4，该环氧化物引发剂如在相关的烯二炔迪尼米星中所发现的那样。令人惊讶的是，发现它相对稳定。在p -氨基取代不利于环氧溶剂分解到原来预想的程度。发现一种弱酸，对甲苯磺酸吡啶鎓，可诱导4的溶剂分解，并导致形成环芳香化产物25。
• Novel Non-nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones as Potent Inhibitors of Both Wild-Type and Cysteine-181 HIV-1 Reverse Transcriptase Enzymes
  作者：John R. Proudfoot、Karl D. Hargrave、Suresh R. Kapadia、Usha R. Patel、Karl G. Grozinger、Daniel W. McNeil、Ernest Cullen、Mario Cardozo、Liang Tong

  DOI：10.1021/jm00024a010

  日期：1995.11

  The major cause of viral resistance to the potent human immunodeficiency virus type 1 reverse transcriptase (RT) inhibitor nevirapine is the mutation substituting cysteine for tyrosine-181 in RT (Y181C RT), An evaluation, against Y181C RT, of previously described analogs of nevirapine revealed that the 2-chlorodipyridodiazepinone 16 is an effective inhibitor of this mutant enzyme. The detailed examination of the structure-activity relationship of 2-substituted dipyridodiazepinones presented below shows that combined activity against the wildtype and Y181C enzymes is achieved with aryl substituents at the 2-position of the tricyclic ring system. In addition, the substitution pattern at C-4, N-5, and N-11 of the dipyridodiazepinone ring system optimum for inhibition of both wild-type and Y181C RT is no longer the 4-methyl-11-cyclopropyl substitution preferred against the wild-type enzyme but rather the 5-methyl-11-ethyl (or 11-cyclopropyl) pattern. The more potent 8-substituted dipyridodiazepinones were evaluated against mutant RT enzymes (L100I RT, K103N RT, P236L RT, and E138K RT) that confer resistance to other non-nucleoside RT inhibitors, and compounds 42, 62, and 67, with pyrrolyl, aminophenyl, and aminopyridyl substituents, respectively, at the 2-position, were found to be effective inhibitors of these mutant enzymes also.
• Biarylpropylsulfonamides as Novel, Potent Potentiators of 2-Amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic Acid (AMPA) Receptors
  作者：Paul L. Ornstein、Dennis M. Zimmerman、M. Brian Arnold、Thomas J. Bleisch、Buddy Cantrell、Richard Simon、Hamideh Zarrinmayeh、S. Richard Baker、Mary Gates、Joseph P. Tizzano、David Bleakman、Allan Mandelzys、Kieth R. Jarvie、Ken Ho、Michelle Deverill、Rajender K. Kamboj

  DOI：10.1021/jm0002836

  日期：2000.11.1
• Sulfonamide derivatives
  申请人：Eli Lilly and Company

  公开号：US06500865B1

  公开（公告）日：2002-12-31

  The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

  本发明提供了某些磺胺类衍生物，可用于增强哺乳动物的谷氨酸受体功能，因此，可用于治疗各种疾病，如精神疾病和神经系统疾病。