1-丙酰吡咯烷-2,5-二酮 | 38614-32-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 1-丙酰吡咯烷-2,5-二酮
• 英文名称: 1-propionylpyrrolidine-2,5-dione
• 英文别名: N-propionyloxysuccinimide；N-propionyl-succinimide；N-propanoylsuccinimide；N-Propionylsuccinimide；1-propanoylpyrrolidine-2,5-dione
• CAS: 38614-32-3
• 化学式: C₇H₉NO₃
• mdl: MFCD00050405
• 分子量: 155.153
• InChiKey: MQOAPJYYLUSVPA-UHFFFAOYSA-N

物化性质

• 沸点：
  254.3±23.0 °C(Predicted)
• 密度：
  1.287±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.571
• 拓扑面积：
  54.4
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2925190090

反应信息

• 作为反应物：
  描述：

  α-D-galactosamine 1-phosphate 、 1-丙酰吡咯烷-2,5-二酮 在 氢氧化钾 作用下， 以 四氢呋喃 、 水 为溶剂， 以90%的产率得到2-deoxy-2-propionylamido-α-D-galactopyranosyl phosphate
  参考文献：
  名称：

  Syntheses of unnatural N-substituted UDP-galactosamines as alternative substrates for N-acetylgalactosaminyl transferases

  摘要：

  UDP-GalNAc analogues with slight modifications in the 2-acetamido group of the GalNAc moiety are prepared in order to study their role in the mechanism of the N-acetylgalactosaminyl transferase mediated glycosylation step. The analogues with N-propionyl, N-butyryl- and N-bromoacetyl-groups were synthesized, utilizing Khorana's morpholidate coupling method starting from D-galactosaminyl-l-phosphate after selective N-acylation of its amino group with the appropriate N-acyloxysuccinimides. Furthermore. in addition to UDP-galactosamine its 2-azido analogue has been efficiently prepared involving a metal catalyzed diazo transfer reaction. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0008-6215(02)00183-0
• 作为产物：
  描述：

  丁二酰亚胺 、 丙酰氯 在 4-二甲氨基吡啶 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以56%的产率得到1-丙酰吡咯烷-2,5-二酮
  参考文献：
  名称：

  N-酰基和N-氨基甲酰基琥珀酰亚胺的合成、X射线晶体学和反应

  摘要：

  摘要 通过琥珀酰亚胺与酰氯的酰化或羧酸的二氯乙烷 (EDC) 偶联制备了一系列 N-酰基和 N-氨基甲酰基琥珀酰亚胺。确定了 N-苯甲酰基和 Np-硝基苯甲酰基琥珀酰亚胺的 X 射线晶体结构。N-酰基琥珀酰亚胺可有效地酰化伯胺、仲胺和芳香胺。补充材料可用于本文。转至出版商的 Synthetic Communications® 在线版以查看免费的补充文件。图形概要

  DOI：

  10.1080/00397911.2012.690061

文献信息

• Some unusual reactivities in the SmI2-mediated reductive coupling of acrylamides and acrylates with imides
  作者：Rolf H. Taaning、Karl B. Lindsay、Troels Skrydstrup

  DOI：10.1016/j.tet.2009.10.089

  日期：2009.12

  A serendipitous discovery of some intra-molecular enolate addition reactions following a SmI2-mediated reductive cross-coupling between imides and electron-deficient olefins leading to some novel compounds was investigated to determine the generality of the protocol and the possible mechanistic pathways involved. This provided a Z-selective synthesis of γ-ketoenediamides in good yields, albeit as of

  研究了酰亚胺和电子不足的烯烃之间由SmI 2介导的还原性交叉偶联后导致一些新型化合物的一些分子内烯醇式加成反应的偶然发现，以确定该方案的一般性和涉及的可能机理。这提供了高产率的γ-酮二酰胺的Z-选择性合成，尽管到目前为止底物的范围仍然有限。还显示，看似相似的丙烯酸酯底物与SmI 2中相应的丙烯酰胺相比，其行为可能有所不同介导的与酰亚胺的还原性交叉偶联反应，有人认为，这些发散的反应性受丙烯酸酯与to金属中心配位的能力支配。
• [³H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H₄ Receptors
  作者：Edith Bartole、Timo Littmann、Miho Tanaka、Takeaki Ozawa、Armin Buschauer、Günther Bernhardt

  DOI：10.1021/acs.jmedchem.9b01342

  日期：2019.9.12

  potential "cold" form of a tritiated H4R ligand. After radiolabeling, binding studies with [3H]UR-DEBa176 ([3H]46) at the h/m/rH4Rs revealed comparable Kd values (41/17/22 nM), low nonspecific binding (11-17%, ∼Kd), and fast associations/dissociations (25-30 min) and disclosed [3H]UR-DEBa176 as useful molecular tool to determine h/m/rH4R binding affinities for H4R ligands.

  人类（h），小鼠（m）和大鼠（r）组胺H4受体（H4R）之间的序列同源性差异会导致配体亲和力，效能和/或效率存在差异，因此会损害翻译动物模型和放射性配体的适用性。针对能够在h / m / rH4Rs上进行稳健和比较结合研究的放射性配体，合成了2,4-二氨基嘧啶并进行了药理研究。鉴定出的最值得注意的化合物是在h / m / rH4R处具有类似效价的两种（部分）激动剂：UR-DEBa148（N-neopentyl-4-（1,4,6,7-tetrahydro-5H-咪唑[4,5 -c] pyridin-5-yl）pyrimidin-2-amine bis（2,2,2-trifluoroacetate），43），最有效的[pEC50（报告基因测定）= 9.9 / 9.6 / 10。3]系列中的化合物略有G蛋白偏置，UR-DEBa176 [[R] -4- [3-（二甲基氨基）吡咯烷丁-1-基] -N-新戊基嘧啶丁-2-胺双（2
• PROCESS FOR THE PREPARATION OF HEXANITROHEXAAZAISOWURTZITANES
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0919556A1

  公开（公告）日：1999-06-02

  A nitro group-containing hexaazaisowurtzitane derivative represented by the following general formula (): wherein n is an integer of 4 or 5, A is an acyl group having 1 - 10 carbon atoms with each acyl group being the same as or different from one or more of the others, N is a nitro group and W is a hexavalent hexaazaisowurtzitane residue represented by the following formula (): a nitroso group-containing hexaazaisowurtzitane derivative represented by the following general formula (): wherein n is an integer of 4 or 5, A is an acyl group having 1 - 10 carbon atoms with each acyl group being the same as or different from one or more of the others, NS is a nitroso group and W is a hexavalent hexaazaisowurtzitane residue of formula () above, and a nitroso group-containing hexaazaisowurtzitane derivative represented by the following general formula (): wherein m is an integer of 4 - 6, A is an acyl group having 1 - 10 carbon atoms with each acyl group being the same as or different from one or more of the others, H is a hydrogen atom and W is a hexavalent hexaazaisowurtzitane residue of formula () above, and a process for preparing hexanitrohexaazaisowurtzitane represented by the following formula (): wherein N is a nitro group and W is a hexavalent hexaazaisowurtzitane residue of formula () above, by nitrating one of said derivatives with a nitrating agent.

  由以下通式（）代表的含硝基六氮唑麝香草烷衍生物： 其中 n 是 4 或 5 的整数，A 是具有 1 - 10 个碳原子的酰基，每个酰基与一个或多个其他酰基相同或不同、 N 是硝基，W 是由下式（）表示的六价六氮杂环戊烷残基： 由下式通式（）代表的含亚硝基六氮唑麝香草烷衍生物： 其中 n 是 4 或 5 的整数，A 是具有 1-10 个碳原子的酰基，每个酰基与一个或多个其他酰基相同或不同、 NS 是亚硝基，W 是上式（）的六价六氮杂昭乌齐坦残基，以及 由以下通式()代表的含亚硝基基团的六氮杂环戊烷衍生物： 其中 m 是 4 - 6 的整数，A 是具有 1 - 10 个碳原子的酰基，每个酰基与一个或多个 其他酰基相同或不同，H 是氢原子，W 是上述式（）的六价六氮杂脲zitane 残基，以及 制备下式()代表的六硝基六氮唑脲的工艺： 其中 N 为硝基，W 为上式（）的六价六氮杂脲zitane 残留物、 用硝化剂将上述衍生物之一硝化。
• NUCLEIC ACID DELIVERY CARRIER, NUCLEIC ACID DELIVERY KIT, AND NUCLEIC ACID DELIVERY METHOD
  申请人：Keio University

  公开号：EP3308789A1

  公开（公告）日：2018-04-18

  The purpose of the present invention is to provide a nucleic acid delivery carrier, a nucleic acid delivery kit, and a nucleic acid delivery method which have an excellent effect of inhibiting cell death after nucleic acid delivery and have excellent efficiency of delivering nucleic acids into cells. This carrier for delivery of nucleic acids into cells comprises a liposome having a membrane fusion capability, wherein the liposome includes a cationic lipid as a membrane constituent, and the surface of the liposome is modified with a temperature-responsive polymer. This nucleic acid delivery carrier is optimally used to deliver nucleic acids into cervical cancer cells. This kit for delivering nucleic acids into cells includes the aforementioned delivery carrier. The nucleic acid delivery method for delivering nucleic acids into cells involves a step for contacting isolated cells with a complex of the aforementioned nucleic acid delivery carrier and nucleic acids, or, a step for dosing a non-human animal with a complex of the aforementioned nucleic acid delivery carrier and nucleic acids.

  本发明的目的是提供一种核酸递送载体、核酸递送试剂盒和核酸递送方法，该核酸递送载体、核酸递送试剂盒和核酸递送方法具有极佳的抑制核酸递送后细胞死亡的效果，并且具有极佳的将核酸递送到细胞中的效率。这种将核酸送入细胞的载体包括具有膜融合能力的脂质体，其中脂质体包括作为膜成分的阳离子脂质，脂质体的表面用温度响应聚合物修饰。这种核酸递送载体最适合用于向宫颈癌细胞递送核酸。这种将核酸递送到细胞中的试剂盒包括上述递送载体。将核酸递送到细胞中的核酸递送方法包括将分离的细胞与上述核酸递送载体和核酸的复合物接触的步骤，或将上述核酸递送载体和核酸的复合物给非人类动物服药的步骤。
• Cell-penetrating compstatin analogs and uses thereof
  申请人：Apellis Pharmaceuticals, Inc.

  公开号：US10308687B2

  公开（公告）日：2019-06-04

  In some aspects, the present invention cell-penetrating compstatin analog and compositions comprising cell-penetrating compstatin analog. In some aspects, the invention further provides methods of using cell-penetrating compstatin analogs treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ, to inhibit production or release of biologically active C3 cleavage products.

  在某些方面，本发明细胞穿透性 compstatin 类似物和包含细胞穿透性 compstatin 类似物的组合物。在某些方面，本发明进一步提供了使用细胞穿透性compstatin类似物治疗补体介导的疾病的方法，例如，抑制补体介导的对细胞、组织或器官的损伤，抑制生物活性C3裂解产物的产生或释放。