tert-butyl 1-(pyridin-3-yl)hydrazinecarboxylate | 1075749-79-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: tert-butyl 1-(pyridin-3-yl)hydrazinecarboxylate
• 英文别名: N-pyridin-3-yl-hydrazinecarboxylic acid tert-butyl ester；tert-butyl N-amino-N-pyridin-3-ylcarbamate
• CAS: 1075749-79-9
• 化学式: C₁₀H₁₅N₃O₂
• 分子量: 209.248
• InChiKey: NYYDVCCHFXPEMP-UHFFFAOYSA-N

物化性质

• 沸点：
  314.7±34.0 °C(Predicted)
• 密度：
  1.179±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  68.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 1-(pyridin-3-yl)hydrazinecarboxylate 在 盐酸 作用下， 以 1,4-二氧六环 为溶剂， 反应 12.0h， 以26.5 g的产率得到3-肼基吡啶盐酸盐
  参考文献：
  名称：

  EP2674423

  摘要：

  公开号：
• 作为产物：
  描述：

  3-碘吡啶 、 肼基甲酸叔丁酯 在 copper(l) iodide 、 caesium carbonate 作用下， 以 二甲基亚砜 为溶剂， 反应 5.0h， 以91%的产率得到tert-butyl 1-(pyridin-3-yl)hydrazinecarboxylate
  参考文献：
  名称：

  CuI / 4-羟基-1-脯氨酸是一种更有效的催化体系，用于将芳族溴化物与N- Boc肼和氨水偶联

  摘要：

  CuI / 4-羟基-1-脯氨酸催化的芳基溴化物与N- Boc肼的偶合反应在DMSO中于80°C进行，得到N-芳基酰肼。当使用芳基碘化物时，该反应在50℃下完成并且不需要配体。在CuI / 4-羟基-1-脯氨酸的催化下，氨水与芳基溴化物的偶联反应在50℃下顺利进行，得到伯芳基胺。在这种情况下，发现K 2 CO 3是比Cs 2 CO 3更好的碱。这些过程允许组装N带有多种官能团的-芳基酰肼和伯芳基胺包括羟基，胺基，三氟甲基，酯基，硝基和酮。

  DOI：

  10.1021/jo9006738

文献信息

• INDAZOLONE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS
  申请人：Bolin David Robert

  公开号：US20110112147A1

  公开（公告）日：2011-05-12

  Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

  本文提供了公式(I)的化合物，以及其药用盐，其中取代基如规范中所披露。这些化合物及含有它们的药物组合物对于治疗代谢性疾病和紊乱，例如II型糖尿病等，具有用处。
• Continuous flow synthesis of arylhydrazines <i>via</i> nickel/photoredox coupling of <i>tert</i>-butyl carbazate with aryl halides
  作者：Alejandro Mata、Duc N. Tran、Ulrich Weigl、Jason D. Williams、C. Oliver Kappe

  DOI：10.1039/d0cc06787c

  日期：——

  Nickel/photoredox catalyzed C–N couplings of hydrazine-derived nucleophiles provide a powerful alternative to Pd-catalyzed methods. This continuous-flow photochemical protocol, optimized using design of experiments, achieves these couplings in short residence times, with high selectivity. A range of (hetero)aryl bromides and chlorides are compatible and understanding of process stability/reactor fouling

  镍/光氧化还原催化的肼衍生亲核试剂的C–N偶联为Pd催化方法提供了有力的替代方法。通过实验设计优化的这种连续流光化学方案可在短停留时间内以高选择性实现这些偶联。一系列（杂）芳基溴化物和氯化物是相容的，并且已经理解了对工艺稳定性/反应器结垢的理解。
• PYRAZOLE DERIVATIVES AND PESTICIDES
  申请人：Numata Akira

  公开号：US20130338367A1

  公开（公告）日：2013-12-19

  Novel pesticide, especially insecticides or miticides are provided. Pyrazole derivative and pesticides represented by the formula (1): wherein A 1 is —N(O) m2 or —CR 1 , each of R 1 , R 3 , R 4 is a hydrogen atom, a halogen atom, C 1 -C 6 alkyl or the like, R a is a hydrogen atom, C 1 -C 6 alkyl or the like, R b is —C(O)R 7 , —C(O)N(R 8a )R 8 or the like, each of R 7 , R 8 , R 8a is a hydrogen atom, C 1 -C 6 alkyl or the like, and m1 is an integer of 0 or 1.

  提供一种新型农药，特别是杀虫剂或杀螨剂。该农药是由吡唑衍生物和式（1）所代表的农药组成：其中A1为—N(O)m2或—CR1，R1、R3、R4分别为氢原子、卤素原子、C1-C6烷基或类似基团，Ra为氢原子、C1-C6烷基或类似基团，Rb为—C(O)R7、—C(O)N(R8a)R8或类似基团，R7、R8、R8a分别为氢原子、C1-C6烷基或类似基团，m1为0或1的整数。
• Design and synthesis of 2-N-substituted indazolone derivatives as non-carboxylic acid glycogen synthase activators
  作者：Yimin Qian、David Bolin、Karin Conde-Knape、Paul Gillespie、Stuart Hayden、Kuo-Sen Huang、Andrée R. Olivier、Tsutomu Sato、Qing Xiang、Weiya Yun、Xiaolei Zhang

  DOI：10.1016/j.bmcl.2013.03.049

  日期：2013.5

  Glycogen synthase (GS) catalyzes the transfer of glucose residues from UDP-glucose to a glycogen polymer chain, a critical step for glucose storage. Patients with type 2 diabetes normally exhibit low glycogen levels and decreased muscle glucose uptake is the major defect in whole body glucose disposal. Therefore, activating GS may provide a potential approach for the treatment of type 2 diabetes. In order to identify non-carboxylic acids GS activators, we designed and synthesized a series of 2-N-alkyl- and 2-N-aryl-indazolone derivatives and studied their activity in activating human GS. (C) 2013 Elsevier Ltd. All rights reserved.
• Copper(I)-picolinic acid catalyzed N-arylation of hydrazides
  作者：Miu Suen Lam、Hang Wai Lee、Albert S.C. Chan、Fuk Yee Kwong

  DOI：10.1016/j.tetlet.2008.08.050

  日期：2008.10

  An efficient copper-catalyzed carbon-nitrogen bond formation is described. The copper(I) complex with commercially available 2-picolinic acid ligand was found to be effective in N-arylation of N-Boc-hydrazine. This methodology offers a regioselective N-arylation of hydrazides using a variety of substituted aryl iodides. (C) 2008 Elsevier Ltd. All rights reserved.