Sarkosylglycin-methylamid | 64642-20-2

• 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: Sarkosylglycin-methylamid
• 英文别名: 2-(methylamino)-N-[2-(methylamino)-2-oxoethyl]acetamide
• CAS: 64642-20-2
• 化学式: C₆H₁₃N₃O₂
• mdl: MFCD11637508
• 分子量: 159.188
• InChiKey: IZCVODDIXKCMAL-UHFFFAOYSA-N

物化性质

• 沸点：
  435.7±30.0 °C(Predicted)
• 密度：
  1.073±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  70.2
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  Methyl-[(methylcarbamoylmethyl-carbamoyl)-methyl]-carbamic acid benzyl ester 生成 Sarkosylglycin-methylamid
  参考文献：
  名称：

  Synthesis of Di- and Tri-substituted 2,4-Dioxo-1,3,2-diazaphospholidines and 4-Oxo-2-thioxo-1,3,2-diazaphospholidines

  摘要：

  DOI：

  10.1055/s-1977-24451

文献信息

• BENZAZEPINE DERIVATIVES USEFUL AS VASOPRESSIN ANTAGONISTS
  申请人：Kondo Kazumi

  公开号：US20110071084A1

  公开（公告）日：2011-03-24

  The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R 1 represents a —CO—(CH 2 ) n —COR 2 group (wherein n is an integer of 1 to 4, and R 2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxo-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

  本发明提供了一种苯哌啶化合物，可以长时间维持托瑞那汀的血药浓度，从而实现所需的药效。本发明的苯哌啶化合物由通式（1）表示，其中R1代表一个—CO—(CH2)n—COR2基团（其中n为1至4的整数，R2为(2-1)一个羟基；(2-2)一个可选择地取代有羟基、较低烷氧基、较低烷酰基、较低烷酰氧基、较低烷氧羰氧基、环烷氧羰氧基或5-甲基-2-氧代-1,3-二氧代-4-基的较低烷氧羰氧基；或(2-3)一个可选择地取代有羟基较低烷基基团的氨基），等等。
• Benzazepine Derivatives Useful as Vasopressin Antagonists
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：US20140024640A1

  公开（公告）日：2014-01-23

  The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R 1 represents a —CO—(CH 2 ) n —COR 2 group (wherein n is an integer of 1 to 4, and R 2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.

  本发明提供了一种苯并氮杂环化合物，可以长时间维持托瑞普坦的血药浓度，从而实现所需的药效。本发明的苯并氮杂环化合物由通式（1）表示，其中R1表示一个—CO—(CH2)n—COR2基团（其中n是1至4的整数，R2是(2-1)一个羟基；(2-2)一个较低的烷氧基，可选地取代一个羟基，一个较低的酰基，一个较低的酰氧基，一个较低的烷氧羰氧基，一个环烷基氧羰氧基，或5-甲基-2-氧代-1,3-二氧杂环戊-4-基）等。
• AMINO MERCAPTAN COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF IN PROTECTION AGAINST RADIATION
  申请人：Inst Of Radiation Medicine Chinese Acad Of Medical Sciences

  公开号：EP3508476A1

  公开（公告）日：2019-07-10

  The present invention discloses an amino mercaptan compound, preparation method thereof and use thereof in radiation protection. The compound has the structure of formula I, wherein A1 is selected from -C(O)NR8-,-S(O)2-NR8-, -S(O)NR8 or -R7-NR8-; A2 is selected from carbonyl, sulfonyl, sulfinyl, substituted or unsubstituted C1-6 alkyl; R1, R2, R5, and R6 may be the same or different and are selected from: hydrogen, substituted or unsubstituted C1-C5 alkyl or heteroalkyl; n is an integer from 0 to 20,000; R3 and R4 are independently selected from hydrogen, X, substituted or unsubstituted C1-6 alkyl; X is selected from F, Cl, Br or I; R7 is selected from substituted or unsubstituted C1-C6 alkyl; and R8 is selected from hydrogen, substituted or unsubstituted C1-C6 alkyl. The compound has the effects of reducing the biological damage caused by ionizing radiation, extending the survival period and survival rate of the radiated animals, and significantly alleviating the side effects of radiotherapy, and has a low toxicity. The present invention opens up a new way for protection and treatment of ionizing radiation damage.

  本发明公开了一种氨基硫醇化合物、其制备方法及其在辐射防护中的用途。该化合物具有式 I 的结构，其中 A1 选自 -C(O)NR8-、-S(O)2-NR8-、-S(O)NR8 或 -R7-NR8-；A2 选自羰基、磺酰基、亚磺酰基、取代或未取代的 C1-6 烷基；R1、R2、R5 和 R6 可以相同或不同，并且选自：氢、取代或未取代的 C1-C5 烷基或杂烷基；n 是 0 至 20,000 的整数；R3 和 R4 独立地选自氢、X、取代或未取代的 C1-6 烷基；X 选自 F、Cl、Br 或 I；R7 选自取代或未取代的 C1-C6 烷基；R8 选自氢、取代或未取代的 C1-C6 烷基。该化合物具有减轻电离辐射造成的生物损伤、延长受辐射动物的存活期和存活率、显著减轻放疗副作用等作用，且毒性低。本发明为电离辐射损伤的防护和治疗开辟了一条新途径。
• Benzazepine derivatives useful as vasopressin antagonists
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP2374798B1

  公开（公告）日：2013-09-04
• US8669229B2
  申请人：——

  公开号：US8669229B2

  公开（公告）日：2014-03-11