ethyl 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylate | 1000784-35-9

• 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: ethyl 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylate
• 英文别名: ethyl 3-hydrazinyl-2,5-dioxopyrrolidine-3-carboxylate
• CAS: 1000784-35-9
• 化学式: C₇H₁₁N₃O₄
• 分子量: 201.182
• InChiKey: VJPCUPKMUMELLJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  111
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  ethyl 3-[N,N'-bis(benzyloxycarbonyl)hydrazino]-2,5-dioxopyrrolidine-3-carboxylate 在 5percent palladium-carbon ethylenediamine complex 氢气 作用下， 以 乙醇 为溶剂， 20.0 ℃ 、101.33 kPa 条件下， 反应 2.5h， 以100%的产率得到ethyl 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylate
  参考文献：
  名称：

  3-HYDRAZINO-2,5-DIOXOPYRROLIDINE-3-CARBOXYLATES, PROCESS FOR PRODUCTION OF THE SAME, AND USE OF THE SAME

  摘要：

  本发明提供了3-肼基-2,5-二氧吡咯烷-3-羧酸酯的公式(I)： 其中R1是C1-6烷基等，R2是氢原子或COOR3基团，其中R3是叔C4-6烷基，2,2,2-三氯乙基或苯甲基，其中苯环部分可以任选地被一个或两个独立地选自由卤素原子、C1-4烷基、C1-4烷氧基、腈基和硝基组成的组的原子或基团所取代，以及其盐，这些盐是有用的，因为它们可以用作以经济上可行且安全的方式，以较短的工艺过程来制备四氢吡咯[1,2-a]吡嗪-4-螺-3'-吡咯烷衍生物，如Ranirestat，后者是治疗糖尿病并发症的有希望的治疗剂，以及制备该化合物的工艺。

  公开号：

  US20090253917A1

文献信息

• OPTICALLY ACTIVE 3-AMINO-2,5-DIOXOPYRROLIDINE-3-CARBOXYLATE, PROCESS FOR PRODUCTION OF THE COMPOUND, AND USE OF THE COMPOUND
  申请人：Tanaka Daisuke

  公开号：US20090286980A1

  公开（公告）日：2009-11-19

  The present invention provides a compound of the formula (III): wherein R is a C 1-6 alkyl group, as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being a promising therapeutic agent for diabetic complications in a short process, in an economically advantageous manner and in high yields, and the process for preparing the same.

  本发明提供了一种化合物，其化学式为(III): 其中R是C1-6烷基，作为一种新颖的光学活性中间体，用于制备四氢吡咯并[1,2-a]吡嗪-4-螺-3'-吡咯啉衍生物，如Ranirestat，是一种有前途的治疗糖尿病并发症的治疗剂，具有短工艺过程、经济优势和高产率，并提供了制备该化合物的方法。
• 3-HYDRAZINO-2,5-DIOXOPYRROLIDINE-3-CARBOXYLATE, PROCESS FOR PRODUCTION OF THE SAME, AND USE OF THE SAME
  申请人：TANAKA Daisuke

  公开号：US20110201807A1

  公开（公告）日：2011-08-18

  The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R 1 is a C 1-6 alkyl group, etc., R 2 is a hydrogen atom or a COOR 3 group, wherein R 3 is a tert-C 4-6 alkyl group, a 2,2,2-trichloroethyl group or a benzyl group in which the benzene ring moiety may be optionally substituted by one or two atoms or groups independently selected from the group consisting of a halogen atom, a C 1-4 alkyl group, a C 1-4 alkoxy group, a cyano group and a nitro group, and a salt thereof, which are useful as a novel intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and the process for preparing the same.

  本发明提供的公式（I）的3-肼基-2,5-二氧代吡咯烷-3-羧酸盐，其中R1是C1-6烷基，R2是氢原子或COOR3基团，其中R3是tert-C4-6烷基，2,2,2-三氯乙基基团或苄基，在苄环取代基团中，苯环取代基团可以选择地由卤素原子、C1-4烷基、C1-4烷氧基、氰基和硝基中的一个或两个原子或基团独立地取代，并且其盐，这些化合物是制备四氢吡咯并[1,2-a]吡嗪-4-螺-3'-吡咯烷衍生物（例如Ranirestat）的新型中间体，这些衍生物是治疗糖尿病并发症的有前途的治疗剂，具有短的过程时间、经济优势和安全性，并且提供了制备这些化合物的方法。
• 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates, process for production of the same, and use of the same
  申请人：Dainippon Sumitomo Pharma Co., Ltd.

  公开号：US08003808B2

  公开（公告）日：2011-08-23

  The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R1 is a C1-6 alkyl group, etc., R2 is a hydrogen atom or a COOR3 group, wherein R3 is a tert-C4-6 alkyl group, a 2,2,2-trichloroethyl group or a benzyl group in which the benzene ring moiety may be optionally substituted by one or two atoms or groups independently selected from the group consisting of a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a cyano group and a nitro group, and a salt thereof, which are useful as a novel intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and the process for preparing the same.

  本发明提供了式(I)的3-肼基-2,5-二氧代吡咯烷-3-羧酸盐：其中R1是C1-6烷基等，R2是氢原子或COOR3基团，其中R3是叔丁基烷基、2,2,2-三氯乙基基团或苄基基团，其中苯环部分可以选择性地被一或两个原子或基团独立地选自由卤素原子、C1-4烷基、C1-4烷氧基、氰基和硝基的基团取代，以及其盐。这些化合物是制备四氢吡咯并[1,2-a]吡嗪-4-螺-3'-吡咯烷衍生物（如Ranirestat）的新型中间体，在短时间内、经济优惠和安全的方式下，有望成为治疗糖尿病并发症的有前途的治疗剂。同时本发明还提供了制备上述化合物的方法。
• 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylate, process for production of the same, and use of the same
  申请人：Tanaka Daisuke

  公开号：US08389742B2

  公开（公告）日：2013-03-05

  The present invention provides 3-hydrazino-2,5-dioxopyrrolidine-3-carboxylates of the formula (I): wherein R1 is a C1-6 alkyl group, etc., R2 is a hydrogen atom or a COOR3 group, wherein R3 is a tert-C4-6 alkyl group, a 2,2,2-trichloroethyl group or a benzyl group in which the benzene ring moiety may be optionally substituted by one or two atoms or groups independently selected from the group consisting of a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a cyano group and a nitro group, and a salt thereof, which are useful as a novel intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being promising therapeutic agents for diabetic complications in a short process and in an economically advantageous and safe manner, and the process for preparing the same.

  本发明提供了式（I）的3-肼基-2,5-二氧代吡咯烷-3-羧酸酯：其中R1是C1-6烷基等，R2是氢原子或COOR3基团，其中R3是叔丁基烷基，2,2,2-三氯乙基基团或苄基，其中苯环基团可以选择性地被一个或两个原子或基团独立地选自由卤素原子，C1-4烷基，C1-4烷氧基，氰基和硝基的组中的替代，以及其盐。这些化合物是一种新的中间体，用于制备四氢吡咯并[1,2-a]吡嗪-4-螺-3'-吡咯烷衍生物，如Ranirestat，这些衍生物是治疗糖尿病并发症的有前途的治疗剂，具有短流程，经济优势和安全性，并提供了其制备方法。
• US8003808B2
  申请人：——

  公开号：US8003808B2

  公开（公告）日：2011-08-23