9-fluorenylmethoxycarbonyl-α-hydroxyglycine | 176638-02-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 9-fluorenylmethoxycarbonyl-α-hydroxyglycine
• 英文别名: α-(hydroxy)-N-(Fmoc)glycine；N-Fmoc-Gly(OH)；2-(9H-fluoren-9-ylmethoxycarbonylamino)-2-hydroxyacetic acid
• CAS: 176638-02-1
• 化学式: C₁₇H₁₅NO₅
• 分子量: 313.31
• InChiKey: SRSIWDVGZPFBQS-UHFFFAOYSA-N

物化性质

• 沸点：
  584.1±45.0 °C(Predicted)
• 密度：
  1.400±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  23
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  95.9
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  9-fluorenylmethoxycarbonyl-α-hydroxyglycine 在 lithium hydroxide 、 硫酸 作用下， 以 水 、 丙酮 为溶剂， 生成 (RS)-Fmoc-alpha-甲氧基甘氨酸
  参考文献：
  名称：

  α-羟基甘氨酸延伸肽的固相合成-肽酰胺的生物前体

  摘要：

  可以将Fmocα-甲氧基甘氨酸掺入固相肽合成（SPPS）方法中，以在最终脱保护并用含5％H 2 O的三氟乙酸从固相支持物上裂解时得到α-羟基甘氨酸延伸的肽。

  DOI：

  10.1016/s0040-4039(00)75818-7
• 作为产物：
  描述：

  芴甲氧羰酰胺 、 乙醛酸 以 乙酸乙酯 为溶剂， 反应 6.0h， 以73%的产率得到9-fluorenylmethoxycarbonyl-α-hydroxyglycine
  参考文献：
  名称：

  α-羟基甘氨酸延伸肽的固相合成-肽酰胺的生物前体

  摘要：

  可以将Fmocα-甲氧基甘氨酸掺入固相肽合成（SPPS）方法中，以在最终脱保护并用含5％H 2 O的三氟乙酸从固相支持物上裂解时得到α-羟基甘氨酸延伸的肽。

  DOI：

  10.1016/s0040-4039(00)75818-7

文献信息

• Novel cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
  申请人：AVENTIS PHARMA S.A.

  公开号：US20040248884A1

  公开（公告）日：2004-12-09

  The present invention relates to a cyclic urea compound of formula I: 1 as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

  本发明涉及一种公式I:1所定义的环状脲化合物。该发明还涉及其制备过程、包含它的制药组合物以及其作为蛋白激酶抑制剂的制药用途。因此，它可用于预防或治疗能够通过抑制蛋白激酶活性来调节的生理紊乱，如实体瘤。
• Compounds That Inhibit Replication Of Human Immunodeficiency Virus
  申请人：Balzarini Maria Rene Jan

  公开号：US20080076824A1

  公开（公告）日：2008-03-27

  The present invention relates to the discovery of a novel class of compounds that inhibit the replication of human immunodeficiency virus (HIV) and approaches to identify these compounds. More specifically, it has been found that enzymatically prepared alpha-hydroxyglycinamide and synthetically prepared alpha-hydroxyglycinamide inhibit the replication of HIV in human serum. Embodiments include methods to identify modified glycinamide compounds that inhibit HUV, methods to isolate and synthesize modified glycinamide compounds, and therapeutic compositions comprising these compounds.

  本发明涉及一种新型化合物类别的发现，该类化合物能够抑制人类免疫缺陷病毒（HIV）的复制，并提供了鉴定这些化合物的方法。具体来说，发现经酶法制备的α-羟基甘氨酰胺和人工合成的α-羟基甘氨酰胺能够抑制HIV在人血清中的复制。实施例包括鉴定抑制HUV的改性甘氨酰胺化合物的方法，分离和合成改性甘氨酰胺化合物的方法，以及包含这些化合物的治疗组合物。
• Cyclic Urea Compounds, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors
  申请人：PATEK Marcel

  公开号：US20080108654A1

  公开（公告）日：2008-05-08

  The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

  本公开涉及一种公式I的环状脲化合物，如此定义，以及其制备过程，包含该化合物的制药组合物和其作为蛋白激酶抑制剂的药物用途。因此，公式I的化合物对于预防或治疗能够通过抑制蛋白激酶活性调节的生理紊乱，如实体肿瘤，是有用的。
• Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
  申请人：Aventis Pharma SA

  公开号：US07354933B2

  公开（公告）日：2008-04-08

  The present invention relates to a cyclic urea compound of formula I: as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use, as an inhibitor on a protein kinase. Thus, it is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

  本发明涉及一种公式I的环状脲化合物，如本文所定义。该发明还涉及其制备过程、包含它的药物组成物及其作为蛋白激酶抑制剂的药物用途。因此，它可用于预防或治疗能够通过抑制蛋白激酶活性来调节的生理紊乱，如实体肿瘤。
• Cyclic urea compounds, preparation thereof and pharmaceutical use thereof as kinase inhibitors
  申请人：Aventis Pharma S.A.

  公开号：US07825115B2

  公开（公告）日：2010-11-02

  The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

  本发明涉及一种公式I的环状脲化合物，其定义如下，以及其制备过程、包含它的药物组合物和其作为蛋白激酶抑制剂的药物用途。因此，公式I的化合物可用于预防或治疗可通过抑制蛋白激酶活性调节的生理紊乱，如实体肿瘤。