phenylacetyl-amidosulfuric acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: phenylacetyl-amidosulfuric acid
• 英文别名: Phenylacetyl-amidoschwefelsaeure；(2-Phenylacetyl)sulfamic acid
• 化学式: C₈H₉NO₄S
• 分子量: 215.23
• InChiKey: OUVOYWAPMUBWMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  91.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-苯乙酰胺 在 硫酸 、 乙酸酐 作用下， 生成 phenylacetyl-amidosulfuric acid
  参考文献：
  名称：

  A STUDY OF THE REACTIONS OF AMMONIUM SULPHAMATE WITH AMIDES AND UREAS

  摘要：

  从酰胺和硫酸铵磺酸酯制备腈类化合物的方法进行了研究。该方法被发现通常适用，并且在大多数情况下获得了良好的产率。反应的机理涉及氨的释放和铵N-羰基磺酸酯的形成，后者分解为腈类化合物和硫酸氢铵。从尿素中形成胍和异三聚氰酸的机理得到了阐明。确定了甲基、苯基、乙酰基和苯甲酰基对尿素分子反应性的影响。从甲基脲和苯基脲中获得了甲胺和苯胺，以及胍和异三聚氰酸。乙酰脲和苯甲酰脲形成乙腈和苯腈，胍的产率较低，但异三聚氰酸的产率非常高。

  DOI：

  10.1139/v56-214

文献信息

• Substituted N-methylene derivatives of thienamycin sulfoxide and sulfone and their preparation
  申请人：Merck & Co., Inc.

  公开号：EP0001264A1

  公开（公告）日：1979-04-04

  Disclosed are substituted N-methylene derivatives of thienamycin sulfoxide (1, n=1) and sulfone (I, n=2) which may be represented by the following structural formula: wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR' R2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R1 and R2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

  本发明公开了噻喃霉素亚砜（1，n=1）和砜（I，n=2）的取代 N-亚甲基衍生物，其结构式如下： 其中 X 和 Y 选自由氢、R、OR、SR 和 NR' R2 组成的组，其中除其他外，R 是取代或未取代的：烷基、烯基、炔基、环烷基、环烷基烷基、芳基、芳烷基、杂芳基、杂芳基烷基、杂环烷基和杂环烷基；R1 和 R2 是氢或 R。此类化合物及其药学上可接受的盐、醚、酯和酰胺衍生物可用作抗生素。此外，还公开了制备此类化合物的工艺；包含此类化合物的药物组合物；以及治疗方法，包括在需要抗生素效果时施用此类化合物和组合物。
• O-, N- and carboxyl derivatives of thienamycin sulfoxide and sulfone, their preparation and pharmaceuticals containing said compounds
  申请人：Merck & Co., Inc.

  公开号：EP0001265A1

  公开（公告）日：1979-04-04

  Disclosed are O-, N- and substituted carboxyl derivatives of thienamycin sulfoxide (I, n =1) and thienamycin sulfone (I, n=2): wherein n is 1 or 2; R and R are independently selected from hydrogen and acyl; R is, interalia, hydrogen, acyl or alkyl; X is O or NR; and R is, inter alia, hydrogen or a pharmaceutically acceptable salt or ester moiety. Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.

  公开了噻吩霉素亚砜（I，n =1）和噻吩霉素砜（I，n =2）的 O-、N-和取代的羧基衍生物： 其中 n 为 1 或 2；R 和 R 独立选自氢和酰基；R 除其他外为氢、酰基或烷基；X 为 O 或 NR；R 除其他外为氢或药学上可接受的盐或酯分子。此类衍生物可用作抗生素。此外，还公开了制备此类衍生物的工艺、包含此类衍生物的药物组合物以及治疗方法，包括在需要抗生素效果时施用此类衍生物和组合物。
• 6- and 6,6- disubstituted-2-substituted-pen-2-em-3-carboxylic acids; processes for their preparation and pharmaceutical compositions containing such compounds
  申请人：Merck & Co., Inc.

  公开号：EP0002210A1

  公开（公告）日：1979-06-13

  Disclosed are 6- and 6.6-disubstituted-2-substituted-pen-2-em-3-carboxylic acids of the following structure: wherein: R1 and R2 are independently selected from hydrogen, -NHR1' (R1' is H or acyl), alkyl, alkoxyl. aralkyl, aryl. heterocyclyl and heterocycfyl-alkyl: R3 is selected from hydrogen, -R, -OR, -SR. -NR2; R is substituted and unsubstituted alkyl, aryl, aralkyl, hetero-heterocyclyl, or heterocyclylalkyl; n is 0 or 1: when n=1, R3 is not -SR. Such compounds and their pharmaceutically acceptable salt, and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

  本发明公开了具有以下结构的 6-和 6.6-二取代-2-取代-戊-2-烯-3-羧酸： 其中R1和R2独立地选自氢、-NHR1'（R1'为H或酰基）、烷基、烷氧基、芳基、杂环基和杂环烷基：R3 选自氢、-R、-OR、-SR.-NR2；R 是取代和未取代的烷基、芳基、烷基、杂杂环基或杂环烷基；n 是 0 或 1：当 n=1 时，R3 不是 -SR。此类化合物及其药学上可接受的盐和酯衍生物可用作抗生素。此外，还公开了制备此类化合物的工艺、包含此类化合物的药物组合物以及治疗方法，包括在需要抗生素效果时施用此类化合物和组合物。
• 6-(1'-Hydroxyethyl)-3-substituted amino-1-azabicyclo(3.2.0)-hept-2-en-7-one-2-carboxylic acid
  申请人：Merck & Co., Inc.

  公开号：EP0134301A1

  公开（公告）日：1985-03-20

  Disclosed are 6-(1'-hydroxyethyl)-3-substituted amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acids (I) : wherein R' and R" are independently selected from H, substituted and unsubstituted alkyl and aralkyl groups, or together form a substituted or unsubstituted cyclic group. Such compounds and their O- and carboxyl derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds.

  公开了 6-(1'-羟乙基)-3-取代氨基-1-氮杂双环[3.2.0]庚-2-烯-7-酮-2-羧酸 (I) ： 其中，R'和 R "独立地选自 H、取代和未取代的烷基和芳烷基，或共同形成取代或未取代的环状基团。此类化合物及其 O-和羧基衍生物可用作抗生素。还公开了制备此类化合物的工艺和包含此类化合物的药物组合物。
• US3974151A
  申请人：——

  公开号：US3974151A

  公开（公告）日：1976-08-10