Tert-butyl (2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)-2-oxoethyl)carbamate | 130916-10-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Tert-butyl (2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)-2-oxoethyl)carbamate
• 英文别名: tert-butyl N-[2-[[1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl]amino]-2-oxoethyl]carbamate
• CAS: 130916-10-8
• 化学式: C₁₁H₂₂N₂O₆
• 分子量: 278.305
• InChiKey: GDGTXFSXNCLKKO-UHFFFAOYSA-N

物化性质

• 沸点：
  592.3±50.0 °C(Predicted)
• 密度：
  1.259±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.9
• 重原子数：
  19
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  128
• 氢给体数：
  5
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  Tert-butyl (2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)-2-oxoethyl)carbamate 在 盐酸 、 4-二甲氨基吡啶 作用下， 以 1,4-二氧六环 、 二氯甲烷 为溶剂， 反应 0.08h， 生成
  参考文献：
  名称：

  MOLECULAR ASSEMBLY USING BRANCHED AMPHIPHILIC BLOCK POLYMER, AND DRUG TRANSPORTATION SYSTEM

  摘要：

  公开号：

  EP2893924B1
• 作为产物：
  描述：

  Boc-甘氨酰胺 、 三羟甲基氨基甲烷 在 2-乙氧基-1-乙氧碳酰基-1,2-二氢喹啉 作用下， 以82%的产率得到Tert-butyl (2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)-2-oxoethyl)carbamate
  参考文献：
  名称：

  Factors Influencing in Vivo Disposition of Polymeric Micelles on Multiple Administrations

  摘要：

  Lactosome is a polymeric micelle composed of amphiphilic polydepsipeptide, poly(sarcosine)64-block-poly(l-lactic acid)30 (AB-type), which accumulates in solid tumors through the enhanced permeability and retention (EPR) effect. However, lactosome on multiple administrations changed its pharmacokinetics from accumulation in tumors to liver due to the production of antilactosome IgM, which was triggered by the first administration. This phenomenon is called the accelerated blood clearance (ABC). In order to reduce the production of antilactosome IgM, a novel nanoparticle composed of (poly(sarcosine)23)3-block-poly(l-lactic acid)30 (A3B-type) was prepared. The A3B-type lactosome at the second administration showed an in vivo disposition similar to that at the first administration due to suppression of antibody production. This study involving the AB- and A3B-type lactosomes, with variation of conditions, revealed that the high local density of poly(sarcosine) chains of the A3B-type lactosome should relate to the prevention of a polymeric micelle from interacting B-cell receptors.

  DOI：

  10.1021/ml500112u

文献信息

• BRANCHED AMPHIPATHIC BLOCK POLYMER AND MOLECULAR AGGREGATE AND DRUG DELIVERY SYSTEM USING SAME
  申请人：Ozeki Eiichi

  公开号：US20140127132A1

  公开（公告）日：2014-05-08

  Provided is a polymeric micelle pharmaceutical preparation that can increase the ratio of contrast at tumor site to background contrast in a short period of time after administration of a lactosome and can suppress the ABC phenomenon so that the lactosome can be administered more than once within a short span. A branched-type amphiphilic block polymer comprising: a multi-branched hydrophilic block comprising sarcosine; and a hydrophobic block comprising polylactic acid. The branched-type amphiphilic block polymer, wherein the number of branches of the hydrophilic block is 3. A molecular assembly comprising the branched-type amphiphilic block polymer. The molecular assembly further comprising a linear type amphiphilic block polymer.

  提供的是一种聚合物胶束制药制剂，可以在给予乳状体后的短时间内增加肿瘤部位与背景对比的比例，并且可以抑制ABC现象，使得乳状体可以在短时间内多次给药。包括以下部分的分支型两性块聚合物：包括硫氨酸的多支链亲水块；和包括聚乳酸的疏水块。该分支型两性块聚合物，其中亲水块的支链数为3。包括该分支型两性块聚合物的分子组装体。该分子组装体进一步包括线型两性块聚合物。
• US9295734B2
  申请人：——

  公开号：US9295734B2

  公开（公告）日：2016-03-29
• US9623122B2
  申请人：——

  公开号：US9623122B2

  公开（公告）日：2017-04-18
• US9821078B2
  申请人：——

  公开号：US9821078B2

  公开（公告）日：2017-11-21
• Factors Influencing <i>in Vivo</i> Disposition of Polymeric Micelles on Multiple Administrations
  作者：Eri Hara、Motoki Ueda、Akira Makino、Isao Hara、Eiichi Ozeki、Shunsaku Kimura

  DOI：10.1021/ml500112u

  日期：2014.8.14

  Lactosome is a polymeric micelle composed of amphiphilic polydepsipeptide, poly(sarcosine)64-block-poly(l-lactic acid)30 (AB-type), which accumulates in solid tumors through the enhanced permeability and retention (EPR) effect. However, lactosome on multiple administrations changed its pharmacokinetics from accumulation in tumors to liver due to the production of antilactosome IgM, which was triggered by the first administration. This phenomenon is called the accelerated blood clearance (ABC). In order to reduce the production of antilactosome IgM, a novel nanoparticle composed of (poly(sarcosine)23)3-block-poly(l-lactic acid)30 (A3B-type) was prepared. The A3B-type lactosome at the second administration showed an in vivo disposition similar to that at the first administration due to suppression of antibody production. This study involving the AB- and A3B-type lactosomes, with variation of conditions, revealed that the high local density of poly(sarcosine) chains of the A3B-type lactosome should relate to the prevention of a polymeric micelle from interacting B-cell receptors.