N-(2,3-二羟基-1-苯基丙基)苯甲酰胺 | 101293-71-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-(2,3-二羟基-1-苯基丙基)苯甲酰胺
• 英文名称: N-(2,3-dihydroxy-1-phenylpropyl)benzamide
• 英文别名: N-(2,3-dihydroxy-1-phenyl-propyl)-benzamide；N-(2,3-Dihydroxy-1-phenyl-propyl)-benzamid；1-Benzamino-1-phenyl-propandiol-(2.3)；N-[(1RS,2RS)-2,3-dihydroxy-1-phenylpropyl]benzamide
• CAS: 101293-71-4
• 化学式: C₁₆H₁₇NO₃
• 分子量: 271.316
• InChiKey: OCRUDDLKDFDNGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  20
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  69.6
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-(2,3-二羟基-1-苯基丙基)苯甲酰胺 在 4-二甲氨基吡啶 、 sodium periodate 、 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 28.0h， 生成 [(1S,2S)-2-benzamido-1-diethoxyphosphoryl-2-phenylethyl] (2S)-2-methoxy-2-phenylacetate
  参考文献：
  名称：

  Enantiomeric phosphonate analogs of the paclitaxel C-13 side chain

  摘要：

  Both enantiomers of syn diethyl 2-(benzoylamino)-1-hydroxy-2-phenylethylphosphonate have been obtained by resolution via O-methylmandelate derivatives. Removal of the resolving ester moiety was easily achieved by ammonolysis with no trace of the retro-Abramov reaction. Absolute configurations of the enantiomeric phosphonate analogs were established from H-1 (the Trost model) and P-31 NMR data of the O-methylmandelate derivatives. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0957-4166(99)00206-2
• 作为产物：
  描述：

  (3-苯基环氧乙烷基)甲醇 在 palladium on activated charcoal 4-二甲氨基吡啶 、 sodium azide 、 氢气 、 氯化铵 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 13.0h， 生成 N-(2,3-二羟基-1-苯基丙基)苯甲酰胺
  参考文献：
  名称：

  Enantiomeric phosphonate analogs of the paclitaxel C-13 side chain

  摘要：

  Both enantiomers of syn diethyl 2-(benzoylamino)-1-hydroxy-2-phenylethylphosphonate have been obtained by resolution via O-methylmandelate derivatives. Removal of the resolving ester moiety was easily achieved by ammonolysis with no trace of the retro-Abramov reaction. Absolute configurations of the enantiomeric phosphonate analogs were established from H-1 (the Trost model) and P-31 NMR data of the O-methylmandelate derivatives. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0957-4166(99)00206-2

文献信息

• 5,6-dihydro-4H-1,3-oxa(or thia)zine derivatives, their preparation and
  申请人：Rhone-Poulenc Sante

  公开号：US04994569A1

  公开（公告）日：1991-02-19

  Compounds of formula: ##STR1## in which R.sub.1 denotes 2-indolyl, 2-thienyl, 3-furyl, naphthyl, phenyl, or phenyl substituted with one or two halogen atoms, with alkoxy, alkyl, nitro, acylamino, alkylthio, acyl, trifluoromethoxy, morpholino, piperidino, amino, mono- or dialkylamino or, at the 3- and 4-positions, with methylenedioxy R.sub.2 denotes phenyl or phenyl substituted with one or two halogen atoms, with one or two alkyl radicals, with alkoxy, nitro, trifluoromethyl or hydroxy or, at the 3- and 4-positions, with methylenedioxy and either X denotes oxygen and R.sub.3 denotes phenyl R.sub.4, R.sub.5 and R.sub.6 denote hydrogen, or R.sub.3 and R.sub.4 denote hydrogen, R.sub.5 denotes hydrogen or methyl and R.sub.6 denotes phenyl or one of R.sub.3 and R.sub.4 denotes methyl and the other hydrogen, R.sub.5 denotes hydrogen and R.sub.6 denotes phenyl, or X denotes sulphur, R.sub.3 denotes phenyl and R.sub.4, R.sub.5 and R.sub.6 denote hydrogen; the said acyl, alkyl and alkoxy radicals and acyl, alkyl and alkoxy portions containing 1 to 4 carbon atoms each in a straight or branched chain; and their salts are useful in the treatment and prevention of disorders in which therapy with a cholecystokinin antagonist is indicated.

  式（I）化合物：##STR1## 其中R1表示2-吲哚基、2-噻吩基、3-呋喃基、萘基、苯基或被一个或两个卤素原子、烷氧基、烷基、硝基、酰胺基、烷硫基、酰基、三氟甲氧基、吗啉基、哌啶基、氨基、单或二烷基氨基或3位和4位上的亚甲二氧基取代的苯基；R2表示苯基或被一个或两个卤素原子、一个或两个烷基、烷氧基、硝基、三氟甲基或羟基或3位和4位上的亚甲二氧基取代的苯基；且X表示氧，R3表示苯基，R4、R5和R6表示氢，或者R3和R4表示氢，R5表示氢或甲基，R6表示苯基，或者R3和R4中一个表示甲基，另一个表示氢，R5表示氢，R6表示苯基，或者X表示硫，R3表示苯基，R4、R5和R6表示氢；所述酰基、烷基和烷氧基基团以及酰基、烷基和烷氧基部分各自包含1至4个碳原子，可以是直链或支链；及其盐，在治疗和预防需要胆囊收缩素拮抗剂治疗的疾病中具有用途。
• PARTICULATE DRUG DELIVERY
  申请人：Cheng Jianjun

  公开号：US20080248126A1

  公开（公告）日：2008-10-09

  Methods for efficient preparation of drug-polymer (or oligomer) conjugates which are useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications. The invention additionally provides certain drug-polymer and drug-oligomer conjugates which are useful in the preparation of particles for delivery of the drug in vivo. The invention also provides nanoparticles of this invention prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

  本发明提供了一种有效制备药物-聚合物（或寡聚物）共轭物的方法，该方法可用于制备微粒和纳米粒子，以在体内传递药物进行治疗应用。本发明还提供了某些药物-聚合物和药物-寡聚物共轭物，该共轭物可用于制备体内药物传递的微粒。本发明还提供了通过使用本发明的药物-聚合物/寡聚物共轭物制备的纳米粒子。药物共轭物是在聚合物或寡聚物的聚合过程中形成的，其中药物被用作引发单体聚合形成聚合物和/或寡聚物的引发剂。更具体地说，药物共轭物是通过在适当的开环聚合催化剂和引发剂（药物）的存在下开环聚合环状单体形成的。该方法特别适用于与含有一个或多个羟基或硫醇基团的药物和其他化学物质形成聚合物/寡聚物共轭物。
• PARTICULATE DRUG DELIVERY METHODS
  申请人：The Board of Trustees of the University of Illinois

  公开号：US20150314006A1

  公开（公告）日：2015-11-05

  Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

  提供了用于高效制备药物-聚合物（或低聚物）共轭物的方法，该方法可用于制备微粒和纳米粒子，以便在体内传递药物进行治疗应用。本发明还提供了使用本发明的药物-聚合物/低聚物共轭物制备的纳米粒子。药物共轭物是在聚合物或低聚物的聚合过程中形成的，其中药物被用作引发单体聚合的引发剂，这些单体形成聚合物和/或低聚物。更具体地说，药物共轭物是通过在适当的开环聚合催化剂和引发剂（药物）存在下的环开口聚合反应中形成的。该方法特别适用于形成聚合物/低聚物共轭物与含有一个或多个羟基或硫醇基团的药物和其他化学物质。
• Chloramphenicol (Chloromycetin).¹ V. Synthesis
  作者：John. Controulis、Mildred C. Rebstock、Harry M. Crooks

  DOI：10.1021/ja01175a066

  日期：1949.7
• Acylated diols
  申请人：SQUIBB & SONS INC

  公开号：US02103266A1

  公开（公告）日：1937-12-28