5,6-二氯-1-(5-O-磷羧基-β-D-呋喃核糖基)-1H-苯并咪唑 | 147190-31-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 中文名称: 5,6-二氯-1-(5-O-磷羧基-β-D-呋喃核糖基)-1H-苯并咪唑
• 中文别名: 9H-芴-9-基甲基[6-羟基-5-(羟基甲基)己基]氨基甲酸酯
• 英文名称: 2-(N-Fmoc-4-aminobutyl)-1,3-propanediol
• 英文别名: 9H-fluoren-9-ylmethyl N-[6-hydroxy-5-(hydroxymethyl)hexyl]carbamate
• CAS: 147190-31-6
• 化学式: C₂₂H₂₇NO₄
• 分子量: 369.5
• InChiKey: JQTRZMDYCYLHBT-UHFFFAOYSA-N

物化性质

• 熔点：
  88-90°C
• 溶解度：
  可溶于氯仿（少许）、DMSO（少许）、乙酸乙酯（少许）

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  27
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  78.8
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Solid support reagents for the direct synthesis of 3'-labeled polynucleotides
  申请人：THE PERKIN-ELMER CORPORATION

  公开号：EP0786468A2

  公开（公告）日：1997-07-30

  The compounds of the invention are exemplified by the class of diglycolate synthesis supports particularly useful as support reagents for the direct synthesis of 3'-labeled polynucleotides. Generally, the compounds of the invention have the structure where T is an acid-cleavable hydroxyl protecting group, e.g., 4,4'-dimethoxytrityl; L1 is a linker for connecting a 3'-terminal nitrogen to carbon; L2 and L3 are linkers for connecting oxygen and carbon; W is a solid support, e.g., CPG or polystyrene; L4 is a linker for connecting the solid support to nitrogen; R1 and R2 are nitrogen substituents, e.g., hydrogen, lower alkyl, nitrogen protecting group, or label; and R3 through R7 are carbon substituents, e.g., hydrogen or lower alkyl. In a first particularly preferred embodiment, the synthesis supports of the invention are exemplified by compounds having the structure where DMT is 4,4'-dimethoxytrityl and W is polystyrene. In a second particularly preferred embodiment, the synthesis supports of the invention are exemplified by compounds having the structure where DMT and W are defined above.

  本发明的化合物属于二羟基乙酸酯合成支持物，特别适用于直接合成 3'- 标记的多核苷酸。一般来说，本发明的化合物具有如下结构 其中，T 是可被酸水解的羟基保护基团，如 4,4'-二甲氧基三苯甲基；L1 是连接 3'末端氮和碳的连接体；L2 和 L3 是连接氧和碳的连接体；W 是固体支持物，如 CPG 或聚苯乙烯；L2 和 L3 是连接氧和碳的连接体、R1和R2是氮取代基，如氢、低级烷基、氮保护基团或标签；R3至R7是碳取代基，如氢或低级烷基。在第一个特别优选的实施方案中，本发明的合成支持物以具有以下结构的化合物为例 其中 DMT 为 4,4'-二甲氧基三苯甲基，W 为聚苯乙烯。在第二个特别优选的实施方案中，本发明的合成支持物以具有以下结构的化合物为例 其中 DMT 和 W 定义如上。
• INSULIN ANALOGUES CONTAINING A GLUCOSE-REGULATED CONFORMATIONAL SWITCH
  申请人：Case Western Reserve University

  公开号：EP3270949A2

  公开（公告）日：2018-01-24
• US5736626A
  申请人：——

  公开号：US5736626A

  公开（公告）日：1998-04-07
• [EN] INSULIN ANALOGUES CONTAINING A GLUCOSE-REGULATED CONFORMATIONAL SWITCH<br/>[FR] ANALOGUES DE L'INSULINE CONTENANT UN COMMUTATEUR DE CONFORMATION RÉGULÉ PAR LE GLUCOSE
  申请人：UNIV CASE WESTERN RESERVE

  公开号：WO2016149222A2

  公开（公告）日：2016-09-22

  A two-chain insulin analogue contains an A chain modified by (i) a monomeric glucose-binding element at or near its N terminus and (ii) a B chain modified by at or near its C terminus by an element that reversibly binds to the monomeric glucose-binding element such that this linkage is displaceable by glucose. The monomeric glucose-binding element may be phenylboronic acid derivative (optionally halogenated). The B chain may be modified by a diol-containing element derived from a monosaccharide, disaccharide or oligosaccharide, a non-saccharide diol-containing moiety or a α-hydroxycarboxylate-containing moiety. The analogue can be manufactured by trypsin-mediated semi-synthesis. Formulations can be at strengths U-10 to U-1000 in soluble solutions at pH 7.0-8.0 with or without zinc ions at a molar ratio of 0.0-3.0 ions per insulin analogue monomer. A patient with diabetes mellitus may be treated with subcutaneous, intraperitoneal, or oral administration of a physiologically effective amount of the insulin analogue.