N-benzyloxycarbonyl-DL-β-homoprolinal | 1378239-20-3

• 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: N-benzyloxycarbonyl-DL-β-homoprolinal
• 英文别名: Benzyl 2-(2-oxoethyl)pyrrolidine-1-carboxylate
• CAS: 1378239-20-3
• 化学式: C₁₄H₁₇NO₃
• 分子量: 247.294
• InChiKey: RONFJKMOSBPPKV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  乙烯氧基三甲基硅烷 、 N-carbobenzyloxyproline 在 碘苯二乙酸 、 碘 、 三氟化硼乙醚 作用下， 以 二氯甲烷 为溶剂， 反应 7.0h， 以82%的产率得到N-benzyloxycarbonyl-DL-β-homoprolinal
  参考文献：
  名称：

  Preparation of modified peptides: direct conversion of α-amino acids into β-amino aldehydes

  摘要：

  开发了一种将α-氨基酸转化为β-氨基醛的直接方法，并应用于肽的C末端残基的修饰。该方法在温和条件下进行，产率良好。同时还描述了该方法在制备含有γ-氨基醇单元的小肽方面的应用，这些单元是肽类抗生素类似物的前体。

  DOI：

  10.1039/c2ob25433f

文献信息

• NEUROPEPTIDE-2 RECEPTOR (Y-2R) AGONISTS
  申请人：Danho Waleed

  公开号：US20100069307A1

  公开（公告）日：2010-03-18

  Provided herein are neuropeptide-2 receptor agonists of the formula (I): Y—R 1 —R 2 —X—R 3 —R 4 —R 5 —R 6 —R 7 —R 8 —R 9 —R 10 —R 11 —R 12 —R 13 —R 14 —NH 2 (I), as well as pharmaceutically acceptable salts, derivatives and fragments thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity and diabetes.

  本文提供了公式(I)的神经肽-2受体激动剂：Y—R1—R2—X—R3—R4—R5—R6—R7—R8—R9—R10—R11—R12—R13—R14—NH2(I)，以及其药学上可接受的盐、衍生物和片段，其中取代基如规范中所披露。这些化合物以及包含它们的药物组合物，可用于治疗肥胖症和糖尿病等疾病。
• Chemoenzymatic process for the preparation of iminocyclitols
  申请人：Clapés Saborit Pere

  公开号：US20100009417A1

  公开（公告）日：2010-01-14

  The present invention discloses a chemoenzymatic process for the preparation of an iminocyclitol corresponding to formula (I), (II), (III) or (IV), wherein: R 1 and R 2 are the same or different, and independently selected from the group consisting of: H, OH, hydroxymethyl, methyl, ethyl, butyl, pentyl, hexyl, octyl, isopropyl, isobutyl, 2-methylbutyl, and benzyl; R 3 is selected from the group consisting of: H, hydroxymethyl, hydroxyethyl, ethyl, butyl, pentyl, hexyl, octyl, dodecyl, isobutyl, isopropyl, isopentyl, 2-methylbutyl, benzyl, and phenylethyl; n: 0 or 1; the process comprising: (i) an aldol addition catalyzed by a D -fructose-6-phosphate aldolase enzyme (FSA) and an acceptor aminoaldehyde; and (ii) an intramolecular reductive amination of the addition adduct obtained in step (i) with H 2 , in the presence of a metallic catalyst, optionally being carried out said step (ii) in the presence of an aldehyde of formula R 3 —CHO, wherein R 3 is as defined above.
• US8288132B2
  申请人：——

  公开号：US8288132B2

  公开（公告）日：2012-10-16
• US8299023B2
  申请人：——

  公开号：US8299023B2

  公开（公告）日：2012-10-30
• Preparation of modified peptides: direct conversion of α-amino acids into β-amino aldehydes
  作者：Carlos J. Saavedra、Alicia Boto、Rosendo Hernández

  DOI：10.1039/c2ob25433f

  日期：——

  A direct method for the transformation of α-amino acids into β-amino aldehydes was developed, and applied to the modification of the C-terminal residue of peptides. The method takes place in good yields and under mild conditions. The application of this methodology to the preparation of small peptides with γ-amino alcohol units, which are precursors of analogues of peptaibol antibiotics, is also described.

  开发了一种将α-氨基酸转化为β-氨基醛的直接方法，并应用于肽的C末端残基的修饰。该方法在温和条件下进行，产率良好。同时还描述了该方法在制备含有γ-氨基醇单元的小肽方面的应用，这些单元是肽类抗生素类似物的前体。