(N-Fmoc-N'-methyl hydrazino)-acetic acid t-butyl ester | 276672-53-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: (N-Fmoc-N'-methyl hydrazino)-acetic acid t-butyl ester
• 英文别名: tert-butyl 2-[(9H-fluoren-9-ylmethoxycarbonylamino)-methylamino]acetate
• CAS: 276672-53-8
• 化学式: C₂₂H₂₆N₂O₄
• 分子量: 382.459
• InChiKey: RFEIXWHZIONRGT-UHFFFAOYSA-N

物化性质

• 密度：
  1.178±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  67.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (N-Fmoc-N'-methyl hydrazino)-acetic acid t-butyl ester 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 fmoc-aza-β3-ala
  参考文献：
  名称：

  带有N-氨基-N-甲基甘氨酸间隔基的新型吡咯烷基PNA的合成及核酸结合研究

  摘要：

  使用固相方法合成了两个新的吡咯烷基肽核酸，它们包含胸腺嘧啶修饰的d-或l-脯氨酸和N-氨基-N-甲基甘氨酸间隔区的交替序列。UV和CD滴定以及凝胶结合移位试验表明，高氨苄胸腺嘧啶PNA十聚体均不与它们的互补DNA或RNA结合。认为这是由于不利的二级结构所致，而该二级结构不能被PNA主链中带正电荷的质子化胺所缓解。

  DOI：

  10.1016/s0040-4039(03)00033-9
• 作为产物：
  描述：

  氯甲酸-9-芴基甲酯 在 盐酸 、 甲醇 、 水 、 碳酸氢钠 、 caesium carbonate 、 sodium iodide 作用下， 以 四氢呋喃 、 水 、 甲苯 为溶剂， 反应 38.0h， 生成 (N-Fmoc-N'-methyl hydrazino)-acetic acid t-butyl ester
  参考文献：
  名称：

  [EN] REVERSE-TURN MIMETICS AND METHOD RELATING THERETO
  [FR] MIMETIQUES A ROTATION INVERSE ET PROCEDE ASSOCIE

  摘要：

  公开号：

  WO2005116032A3

文献信息

• 一种Fmoc-Aza-β³-Ala的合成方法
  申请人：杭州瑞岚得医疗科技有限公司

  公开号：CN108178740A

  公开（公告）日：2018-06-19

  本发明公开了一种Fmoc‑Aza‑β 3 ‑Ala的合成方法，所述的方法为：用过量的二碳酸二叔丁酯处理甲基肼得到式B1所示的化合物1，向所得式B1所示的化合物1中加入Fmoc‑cl和NaHCO 3 发生亲核取代得到式B2所示的化合物2，用三氟乙酸(TFA)或HCLG酸化所得式B2所示的化合物2，使Boc保护基团断裂得到式B3所示的化合物3；将所得式B3所示的化合物3与溴乙酸叔丁酯发生亲核取代得到式A4所示的化合物4；将所得式A4所示的化合物4与通有HCl气体的二氯甲烷进行脱脂反应得到式B5所示的目标产物Fmoc‑Aza‑β 3 ‑Ala。本发明所述的制备方法，反应条件温和，Fmoc保护基团可以很容易地使用温和碱性条件除去，操作简便，酸不稳定基团可用于保护侧链，路线简单高效。
• REVERSE-TURN MIMETICS AND METHOD RELATING THERETO
  申请人：Moon Sung Hwan

  公开号：US20100029630A1

  公开（公告）日：2010-02-04

  Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

  本文揭示了具有构象约束的化合物，其模拟生物活性肽和蛋白质的反转区域的二级结构。这种反转区域模拟结构在广泛的领域中具有实用性，包括用作诊断和治疗剂。本发明还揭示了包含这种反转区域模拟结构的文库，以及筛选这些文库以识别具有生物活性成员的方法。本发明还涉及使用这些化合物来抑制或治疗由Wnt信号通路调节的疾病，例如癌症，特别是结肠直肠癌，与血管成形术相关的再狭窄，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化症，阿尔茨海默病，过度生长或脱发，或溃疡性结肠炎。
• Reverse-turn mimetics and method relating thereto
  申请人：Moon Hwan Sung

  公开号：US20070021425A1

  公开（公告）日：2007-01-25

  Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

  本发明揭示了能够模拟生物活性肽和蛋白质的反转区域的二级结构的构象限制化合物。这种反转区域拟态结构在广泛的领域中具有实用性，包括用作诊断和治疗剂。本发明还揭示了包含这种反转区域拟态结构的库，以及筛选这些库以识别生物活性成员的方法。本发明还涉及使用这些化合物来抑制或治疗由Wnt信号通路调节的疾病，例如癌症，特别是结直肠癌，与血管成形术相关的再狭窄，多囊肾病，异常血管生成疾病，类风湿性关节炎疾病，结节性硬化症，阿尔茨海默病，过度生发或脱发，或溃疡性结肠炎。
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ID NO 49 (for SEQ: ID NO 1 as claimed) and SEQ ID NO 2 (for SEQ ID NO 3 as claimed)X70-79,90-96,104-110,116-127,138-144,152-158XUS6063583AMONTMINY MARC R [US]20000516col. 13-30X70-79,90-96,104-110XWO9918124A1MERCK & CO INC [US], et al19990415Wsee esp. Fig. 7aX80-89,97-103,111-117XPATENT ABSTRACTS OF JAPAN vol. 1999, no. 05 31 May 1999 (1999-05-31)PATENT ABSTRACTS OF JAPAN19990531199905JPH1132767AAClaim 3, pp. 13-14, Seq. with 567 amino acidsX80-89,97-103,111-117,128-137,145-151,159-165XWO02065134A2UNIV DUNDEE [GB], et al20020822claim 9, SEQ: ID NO 9X80-89,97-103,111-117XWO9803652A2US HEALTH [US], et al19980129see the whole document. Specifically, Seq ID NO 3 and Seq. ID NO 9, also claims 1-16X80-89,97-103,111-117,128-137,145-151,159-165XEP1302104A1CHUGAI PHARMACEUTICAL CO LTD [JP], et al20030416seq. ID No. 1, example 1X128-137,145-151,159-165X
  申请人：CHOONGWAE PHARMA CORP

  公开号：WO2005021025A3

  公开（公告）日：2005-07-07
• Cheguillaume, Arnaud; Doubli-Bounoua, Ismahel; Baudy-Floc'h, Michèle, Synlett, 2000, # 3, p. 331 - 334
  作者：Cheguillaume, Arnaud、Doubli-Bounoua, Ismahel、Baudy-Floc'h, Michèle、Le Grel, Philippe

  DOI：——

  日期：——