4-benzoylamino-1-methyl-1H-pyrimidin-2-one | 71937-96-7

• 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: 4-benzoylamino-1-methyl-1H-pyrimidin-2-one
• 英文别名: N-(1-methyl-2-oxo-1,2-dihydro-pyrimidin-4-yl)-benzamide；N-(1-Methyl-2-oxo-1,2-dihydro-pyrimidin-4-yl)-benzamid；N-(1-methyl-2-oxopyrimidin-4-yl)benzamide
• CAS: 71937-96-7
• 化学式: C₁₂H₁₁N₃O₂
• 分子量: 229.238
• InChiKey: UJENRKCFOQVRPT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  61.8
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  重氮甲烷 、 4-benzoylamino-1-methyl-1H-pyrimidin-2-one 生成 4-benzoylamino-1,3-dimethyl-2-oxo-1(3),2-dihydro-pyrimidinium-betaine
  参考文献：
  名称：

  Kenner et al., Journal of the Chemical Society, 1955, p. 855,859

  摘要：

  DOI：
• 作为产物：
  描述：

  4-甲氧基-1-甲基嘧啶-2-酮 在 吡啶 、 甲醇 、 氨 作用下， 生成 4-benzoylamino-1-methyl-1H-pyrimidin-2-one
  参考文献：
  名称：

  Kenner et al., Journal of the Chemical Society, 1955, p. 855,859

  摘要：

  DOI：

文献信息

• SYNTHESIS OF MORPHOLINO OLIGOMERS USING DOUBLY PROTECTED GUANINE MORPHOLINO SUBUNITS
  申请人：REEVES MATTHEW DALE

  公开号：US20090131624A1

  公开（公告）日：2009-05-21

  Morpholino compounds are provided having the structure: where R 1 is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl; R 2 is selected from the group consisting of lower alkyl, monocyclic arylmethyl, and monocyclic (aryloxy)methyl; R 3 is selected from the group consisting of triarylmethyl and hydrogen; and Y is selected from the group consisting of: a protected or unprotected hydroxyl or amino group; a chlorophosphoramidate group; and a phosphorodiamidate linkage to the ring nitrogen of a further morpholino compound or a morpholino oligomer. Such compounds include doubly protected morpholino guanine (MoG) monomers. Also described is their use in synthesis of morpholino oligomers.

  Morpholino化合物具有以下结构： 其中 R1选自由较低烷基、二(较低烷基)氨基和苯基组成的群体； R2选自由较低烷基、单环芳基甲基和单环(芳氧基)甲基组成的群体； R3选自由三芳基甲基和氢原子组成的群体；以及 Y选自由受保护或未受保护的羟基或氨基团；氯磷酰胺基团；以及与另一种morpholino化合物或morpholino寡聚体的环氮原子形成磷酰二胺酸酯键的群体。这类化合物包括双保护的morpholino鸟嘌呤（MoG）单体。还描述了它们在morpholino寡聚体合成中的用途。
• [EN] PROCESSES FOR PREPARING OLIGOMERS<br/>[FR] PROCÉDÉS DE PRÉPARATION D'OLIGOMÈRES
  申请人：SAREPTA THERAPEUTICS INC

  公开号：WO2017205496A1

  公开（公告）日：2017-11-30

  Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomersynthesis while maintaining overall yield and purity of a synthesized oligomer.

  本文提供了制备寡聚物（例如吗啉基寡聚物）的过程。本文描述的合成过程可能有利于扩大寡聚物合成规模，同时保持合成寡聚物的总产量和纯度。
• Methods Of Making Pyranopyrans Such As Pyranopyran Nitrile And Methods of Using Pyranopyrans Such As Pyranopyran Nitrile
  申请人：The United States of America, as Represented by the Secretary of Agriculture

  公开号：US20200093132A1

  公开（公告）日：2020-03-26

  Disclosed herein are methods of making (4aR,6S,8aR)-6-((R)-1-hydroxyethyl)-6,8a-dihydropyrano[3,2-b]pyran-2-(4aH)-one (2) and methods of making (4aR,6S,8aR)-6-cyano-6,8a-dihydropyrano-[3,2-b]pyran-2(4aH)-one (4). Other pyranopyrans were also synthesized. Also compositions containing (4aR,6S,8aR)-6-cyano-6,8a-dihydropyrano-[3,2-b]pyran-2(4aH)-one (4) (or other pyranopyrans described herein) and optionally a carrier. In addition, methods for killing microorganisms or weeds on or in an object or area involving contacting the object or area with an effective microorganisms or weeds killing amount of a composition containing (4aR,6S,8aR)-6-cyano-6,8a-dihydropyrano-[3,2-b]pyran-2(4aH)-one (4) (or other pyranopyrans described herein) and optionally a carrier.

  本发明公开了制备(4aR,6S,8aR)-6-((R)-1-羟乙基)-6,8a-二氢吡喃并[3,2-b]吡喃-2-(4aH)-酮(2)的方法以及制备(4aR,6S,8aR)-6-氰基-6,8a-二氢吡喃并[3,2-b]吡喃-2(4aH)-酮(4)的方法。还合成了其他吡喃并吡喃类化合物。还提供了含有(4aR,6S,8aR)-6-氰基-6,8a-二氢吡喃并[3,2-b]吡喃-2(4aH)-酮(4)（或本文所述的其他吡喃并吡喃类化合物）及可选载体的组合物。此外，还提供了杀灭物体或区域上或内的微生物或杂草的方法，该方法涉及将该物体或区域与含有(4aR,6S,8aR)-6-氰基-6,8a-二氢吡喃并[3,2-b]吡喃-2(4aH)-酮(4)（或本文所述的其他吡喃并吡喃类化合物）及可选载体的组合物接触，该组合物具有有效杀灭微生物或杂草的量。
• [EN] PROCESSES FOR PREPARING OLIGONUCLEOTIDES<br/>[FR] PROCÉDÉS DE PRÉPARATION D'OLIGONUCLÉOTIDES
  申请人：CHANGZHOU SYNTHEALL PHARMACEUTICALS CO LTD

  公开号：WO2022006871A1

  公开（公告）日：2022-01-13

  Disclosed are processes for preparing oligonucleotides. The process comprises: (a) converting a compound of Formula X-1 into a compound of Formula X-2: where R10 is a residue of an oligonucleotide (e.g., a phosphorodiamidate morpholino oligomer); R11 is an amine protecting group; wherein the compound of Formula X-1 is not bound to a solid support; and; (b) optionally removing protecting groups in the compound of Formula X-2 to obtain the oligonucleotide. The synthetic processes described herein are advantageous in many aspects, including but not limited to improved yields and purities of target phosphorodiamidate morpholino oligomers with reduced 4-nitrostyrene adduct impurities. (X-1), (X-2)

  公开了制备寡核苷酸的过程。该过程包括：(a)将式X-1的化合物转化为式X-2的化合物：其中R10是寡核苷酸的残基(例如，磷酸二酰胺吗啉寡聚体)；R11是胺保护基；其中式X-1的化合物未结合到固体支持上；以及；(b)可选地去除式X-2的化合物中的保护基，以获得寡核苷酸。本文所描述的合成过程在许多方面具有优势，包括但不限于提高目标磷酸二酰胺吗啉寡聚体的产率和纯度，并减少4-硝基苯乙烯加合物杂质。(X-1)，(X-2)
• Method for the Preparation of Peptide-Oligonucleotide Conjugates
  申请人：Katzhendler Jehoshua

  公开号：US20080221303A1

  公开（公告）日：2008-09-11

  The present invention relates to the synthesis of peptide-oligonucleotide conjugates (POC). More specifically, the invention relates to a novel method for the preparation of peptide-oligonucleotide conjugates, which can be conducted under mild conditions on solid support, can be performed manually or by a synthesizer, can be used to synthesize alternating sequences of peptides and oligonucleotides, and is applicable to the synthesis of a wide variety of peptide-oligonucleotide conjugates constructed from alternate peptide and oligonucleotide blocks.

  本发明涉及肽-寡核苷酸共轭物（POC）的合成。更具体地说，本发明涉及一种新颖的肽-寡核苷酸共轭物的制备方法，可以在固相支持下在温和条件下进行，可以手动或通过合成器进行，可以用于合成肽和寡核苷酸的交替序列，并适用于从交替肽和寡核苷酸块构建的各种肽-寡核苷酸共轭物的合成。