4-(tert-butyl-dimethyl-silanyloxy)-but-2-ynylamine | 596793-88-3

• 分子结构分类: 有机化合物 - 有机金属化合物 - 有机类金属化合物
• 英文名称: 4-(tert-butyl-dimethyl-silanyloxy)-but-2-ynylamine
• 英文别名: 4-(tert-Butyl-dimethylsilanyloxy)-but-2-ynylamine；4-[tert-butyl(dimethyl)silyl]oxybut-2-yn-1-amine
• CAS: 596793-88-3
• 化学式: C₁₀H₂₁NOSi
• 分子量: 199.368
• InChiKey: TWIYTHIQJBIOKE-UHFFFAOYSA-N

物化性质

• 沸点：
  227.0±25.0 °C(Predicted)
• 密度：
  0.895±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.97
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(tert-butyl-dimethyl-silanyloxy)-but-2-ynylamine 在 甲酸铵 、 溶剂黄146 、 锌 作用下， 以 甲醇 、 甲苯 为溶剂， 反应 9.5h， 生成
  参考文献：
  名称：

  （+）-Strychnine的不对称全合成

  摘要：

  公开了用于（+）-金丝氨酸的催化不对称全合成的合成策略。该合成的关键特征包括建立起始手性的手性的有机催化对映选择性迈克尔加成反应，光诱导的自由基级联反应以进入Corynanthe生物碱中间体，以及受生物启发的级联重排以生成Strychnos生物碱的核心。

  DOI：

  10.1021/acs.orglett.8b03686
• 作为产物：
  描述：

  4-azidobut-2-ynoxy-tert-butyl-dimethylsilane 在 三苯基膦 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 48.0h， 以95%的产率得到4-(tert-butyl-dimethyl-silanyloxy)-but-2-ynylamine
  参考文献：
  名称：

  A sequential reaction process to assemble polysubstituted indolizidines, quinolizidines and quinolizidine analogues

  摘要：

  The omega-iodo-alpha,beta-alkynoates and their ketone, sulfone or phosphonate analogues react with delta-chloropropylamines in MeCN assisted with K2CO3 to undergo a sequential S(N)2/Michael addition/S(N)2/S(N)2 reaction process, giving polysubstituted indolizidines or quinolizidines in good to excellent yields. This sequential reaction process is also compatible with three other substituted alpha,beta-alkynoates, affording quinolizidine analogues in moderate to good yields. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2006.03.068

文献信息

• [EN] 2-(1H-INDAZOL-6-YLAMINO)-BENZAMIDE COMPOUNDS AS PROTEIN KINASES INHIBITORS USEFUL FOR THE TREATMENT OF OPHTALMIC DISEASES<br/>[FR] COMPOSES DE 2-(1H-INDAZOL-6-YLAMINO)-BENZAMIDES EN TANT QU'INHIBITEURS DE PROTEINES KINASES UTILES POUR LE TRAITEMENT DE MALADIES OPHTALMIQUES
  申请人：PFIZER

  公开号：WO2004056806A1

  公开（公告）日：2004-07-08

  Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma,rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

  描述了可以调节和/或抑制眼科疾病和某些蛋白激酶活性的吲哚唑化合物。这些化合物和含有它们的药物组合物能够介导酪氨酸激酶信号传导，从而调节和/或抑制不需要的细胞增殖。该发明还涉及含有这些化合物的药物组合物的治疗或预防用途，以及通过给予这些化合物的有效剂量来治疗眼科疾病和癌症以及与不需要的血管生成和/或细胞增殖相关的其他疾病状态，如糖尿病视网膜病变、新生血管性青光眼、类风湿性关节炎和牛皮癣。
• Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
  申请人：Agouron Pharmaceuticals, Inc.

  公开号：US20040192735A1

  公开（公告）日：2004-09-30

  Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

  本文描述了调节和/或抑制眼科疾病和某些蛋白激酶活性的吲唑化合物。这些化合物和含有它们的药物组合物能够介导酪氨酸激酶信号传导，从而调节和/或抑制不必要的细胞增殖。本发明还涉及含有这些化合物的药物组合物的治疗或预防用途，以及通过给予这些化合物的有效量来治疗眼科疾病和与不必要的血管生成和/或细胞增殖相关的癌症和其他疾病状态，如糖尿病视网膜病变、新生血管性青光眼、类风湿性关节炎和银屑病。
• A sequential reaction process to assemble polysubstituted indolizidines, quinolizidines and quinolizidine analogues
  作者：Guorong Cai、Wei Zhu、Dawei Ma

  DOI：10.1016/j.tet.2006.03.068

  日期：2006.6

  The omega-iodo-alpha,beta-alkynoates and their ketone, sulfone or phosphonate analogues react with delta-chloropropylamines in MeCN assisted with K2CO3 to undergo a sequential S(N)2/Michael addition/S(N)2/S(N)2 reaction process, giving polysubstituted indolizidines or quinolizidines in good to excellent yields. This sequential reaction process is also compatible with three other substituted alpha,beta-alkynoates, affording quinolizidine analogues in moderate to good yields. (c) 2006 Elsevier Ltd. All rights reserved.
• Asymmetric Total Synthesis of (+)-Strychnine
  作者：Liping He、Xiaobei Wang、Xiaoqing Wu、Zhaoxiang Meng、Xin Peng、Xiao-Yu Liu、Yong Qin

  DOI：10.1021/acs.orglett.8b03686

  日期：2019.1.4

  A synthetic strategy for the catalytic asymmetric total synthesis of (+)-strychnine is disclosed. Key features of this synthesis include an organocatalytic enantioselective Michael addition to establish the chirality of the starting building block, a photoinduced radical cascade reaction to access the Corynanthe alkaloid intermediate, and a bioinspired cascade rearrangement to generate the core of

  公开了用于（+）-金丝氨酸的催化不对称全合成的合成策略。该合成的关键特征包括建立起始手性的手性的有机催化对映选择性迈克尔加成反应，光诱导的自由基级联反应以进入Corynanthe生物碱中间体，以及受生物启发的级联重排以生成Strychnos生物碱的核心。