(9H-fluoren-9-yl)methyl 2-(hydroxymethyl)morpholine-4-carboxylate | 885953-31-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: (9H-fluoren-9-yl)methyl 2-(hydroxymethyl)morpholine-4-carboxylate
• 英文别名: 9H-fluoren-9-ylmethyl 2-(hydroxymethyl)morpholine-4-carboxylate
• CAS: 885953-31-1
• 化学式: C₂₀H₂₁NO₄
• 分子量: 339.391
• InChiKey: RHLNPNGKORBWJY-UHFFFAOYSA-N

物化性质

• 沸点：
  535.0±40.0 °C(Predicted)
• 密度：
  1.261±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  59
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (9H-fluoren-9-yl)methyl 2-(hydroxymethyl)morpholine-4-carboxylate 在 哌啶 作用下， 以 二氯甲烷 为溶剂， 生成 2-羟甲基吗啉
  参考文献：
  名称：

  Disubstituted pyrimidines as Lck inhibitors

  摘要：

  We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cellular IL2 release. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.07.102
• 作为产物：
  描述：

  9H-fluoren-9-ylmethyl 2-[(2-methoxyacetyl)oxymethyl]morpholine-4-carboxylate 在 sodium tetrahydroborate 作用下， 以 乙醇 为溶剂， 反应 1.0h， 以90%的产率得到(9H-fluoren-9-yl)methyl 2-(hydroxymethyl)morpholine-4-carboxylate
  参考文献：
  名称：

  使用硼氢化钠还原去除甲氧基乙酰基保护基

  摘要：

  在这里，我们已经开发了一种使用硼氢化钠的MAc保护的醇类的温和选择性还原脱保护方法。新的脱保护条件使O -MAc与其他保护基团（例如叔丁酯，N -Boc，Fmoc，Cbz，O -TBDMS，N-苄基，O-苄基，O-乙酰基，N-乙酰基）完全正交。，N -MAc等。除了O -MAc脱保护外，该方法也适用于S -MAc脱保护。

  DOI：

  10.1016/j.tetlet.2013.11.074

文献信息

• [EN] PYRIMIDINE AND PYRIDINE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS<br/>[FR] DÉRIVÉS DE PYRIMIDINE ET DE PYRIDINE ET LEUR UTILISATION PHARMACEUTIQUE ET LEURS COMPOSITIONS
  申请人：PFIZER

  公开号：WO2009016498A1

  公开（公告）日：2009-02-05

  The prsent invention relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.
• Reductive removal of methoxyacetyl protective group using sodium borohydride
  作者：Pradip K. Gadekar、Maryann Hoermann、Faith Corbo、Rajiv Sharma、S. Sarveswari、Abhijit Roychowdhury

  DOI：10.1016/j.tetlet.2013.11.074

  日期：2014.1

  Herein, we have developed a mild and selective reductive deprotection method for the MAc protected alcohols using sodium borohydride. The new deprotection conditions provide a complete orthogonality between O-MAc and other protecting groups such as tert-butyl ester, N-Boc, Fmoc, Cbz, O-TBDMS, N-benzyl, O-benzyl, O-acetyl, N-acetyl, N-MAc, etc. In addition to O-MAc deprotection, this method is also

  在这里，我们已经开发了一种使用硼氢化钠的MAc保护的醇类的温和选择性还原脱保护方法。新的脱保护条件使O -MAc与其他保护基团（例如叔丁酯，N -Boc，Fmoc，Cbz，O -TBDMS，N-苄基，O-苄基，O-乙酰基，N-乙酰基）完全正交。，N -MAc等。除了O -MAc脱保护外，该方法也适用于S -MAc脱保护。
• Disubstituted pyrimidines as Lck inhibitors
  作者：Julianne A. Hunt、Richard T. Beresis、Joung L. Goulet、Mark A. Holmes、Xinfang J. Hong、Ernest Kovacs、Sander G. Mills、Rowena D. Ruzek、Frederick Wong、Jeffrey D. Hermes、Young-Whan Park、Scott P. Salowe、Lisa M. Sonatore、Lin Wu、Andrea Woods、Dennis M. Zaller、Peter J. Sinclair

  DOI：10.1016/j.bmcl.2009.07.102

  日期：2009.9

  We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cellular IL2 release. (C) 2009 Elsevier Ltd. All rights reserved.