Pyridinepropanoic acid | 53088-71-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: Pyridinepropanoic acid
• 英文别名: propanoic acid;pyridine
• CAS: 53088-71-4
• 化学式: C8H11NO2
• 分子量: 153.18
• InChiKey: UINFICGYFFOSMB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.56
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] IMPROVED PROCESS FOR THE PREPARATION OF ENTACAPONE<br/>[FR] PROCEDE AMELIORE DE PREPARATION DE L'ENTACAPONE
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2005063693A1

  公开（公告）日：2005-07-14

  The invention disclosed in this application relates to an improved process for the preparation of the Entacapone which comprises. (i)reacting 3-alkoxy- 4-hydroxy-5-nitrobenzadehyde with N,N-diethylaminocyanoactamide in the presence of mild acid catalyst and a solvent at a temperature in the range of 50-115 °C, to get the 3-O-alkylated (methyl or ethyl) Entacapone and treating with acid catalysts in the presence of organic base and solvents at temperature in the range of 20-60 °C to get Entacapone.

  这份申请中披露的发明涉及一种改进的恩他卡朋的制备过程，包括：(i)在温度范围为50-115°C的条件下，在温和酸性催化剂和溶剂的存在下，将3-烷氧基-4-羟基-5-硝基苯甲醛与N,N-二乙基氨基氰基乙酰胺反应，得到3-O-烷基化（甲基或乙基）恩他卡朋，并在有机碱和溶剂存在的条件下，在20-60°C的温度范围内用酸性催化剂处理，得到恩他卡朋。
• Methods for the preparation of Entacapone
  申请人：Venkateswarlu Jasti

  公开号：US20070060767A1

  公开（公告）日：2007-03-15

  The invention disclosed in this application relates to an improved process for the preparation of Entacapone. In one embodiment the process involves: (i) reacting a 3-alkoxy-4-hydroxy-5-nitrobenzadehyde with N,N-diethylaminocyanoacetamide in the presence of a mild acid catalyst and a solvent, to provide a 3-O-alkylated Entacapone, and treating the 3-O-alkylated Entacapone with an acid catalyst in the presence of an organic base to provide Entacapone.

  这个申请中披露的发明涉及一种改进的恩他卡韦制备工艺。在一个实施例中，该工艺包括：(i) 在温和酸催化剂和溶剂的存在下，将3-烷氧基-4-羟基-5-硝基苯甲醛与N,N-二乙基氨基丙腈反应，得到3-O-烷基化的恩他卡韦，并在有机碱的存在下，用酸催化剂处理3-O-烷基化的恩他卡韦，得到恩他卡韦。
• Process for the preparation and purification of 2-(alkoxyalkylidene)-3-ketoalkanoic acid esters from 3-ketoalkanoic acid esters
  申请人：Draper W. Richard

  公开号：US20050027140A1

  公开（公告）日：2005-02-03

  In its several embodiments, this invention discloses a novel process to prepare the compounds of Formula 3: wherein R 1 is lower alkyl, and R 2 and R 3 can be the same or different, each being independently selected from the group consisting of alkyl, aryl and aralkyl; said process being carried out in a suitable solvent with at least one tert-amine carboxylate salt catalyst. The compounds of formula 3 are chemical intermediates useful for the synthesis of various heterocyclic compounds. These heterocyclic compounds are in turn useful precursors for diverse pharmaceutical, herbicidal and insecticidal agents. In particular, these intermediates are useful precursors to a variety of CCR5 inhibitors.

  在其多个实施例中，本发明揭示了一种制备式3化合物的新型过程：其中R1为低碳基，R2和R3可以相同或不同，每个独立地从由烷基，芳基和芳基烷基组成的群体中选择；该过程在适当的溶剂中以至少一种三甲胺羧酸盐催化剂进行。式3化合物是有用的化学中间体，可用于合成各种杂环化合物。这些杂环化合物反过来是各种药物，除草剂和杀虫剂的有用前体。特别地，这些中间体是各种CCR5抑制剂的有用前体。
• Improvements in the expression of newly introduced genes in yeast cells
  申请人：UNILEVER N.V.

  公开号：EP0129268A2

  公开（公告）日：1984-12-27

  The invention relates to an improved expression system for newly introduced genes in yeast and comprises a yeast regulon, and preferably a transcription terminator, derived from one of the GAPDH genes of S. cerevisiae. The about 850 nucleotides long GAPDH regulon described proved to be almost ten times as effective as smaller regulons described previously. Said regulon and/orterminator can be introduced into yeasts either as part of plasmid molecules or by incorporating into the yeast genome. Vectors containing the expression system preferably comprise an autonomously replicating sequence derived from K. lactis (KARS) or an origin of replication originating from the S. cerevisiae 2 micron yeast plasmid. After transformation of yeasts, in particular of the genera Kluyveromyces and Saccharomyces, with said vectors, the yeasts transformed can produce foreign proteins more effectively. In the case ofthaumatin the presence of signal polypeptide (the pre-part) appears to be essential for expression in yeast. DNA sequence encoding other signal polypeptides are also described. The use of codons preferred by yeast in both structural genes, preferably those encoding thaumatin- like proteins and chymosin-like proteins, and DNA sequences encoding signal polypeptides is also described.

  本发明涉及一种用于酵母中新引入基因的改良表达系统，它包括一个酵母调控子，最好是一个转录终止子，该调控子来自 S. cerevisiae 的 GAPDH 基因之一。事实证明，所述的约 850 个核苷酸长的 GAPDH 调节子的有效性几乎是以前所述的较小调节子的十倍。所述调控子和/或终止子可作为质粒分子的一部分或通过加入酵母基因组导入酵母。 含有表达系统的载体最好是由源自 K. lactis（KARS）的自主复制序列或源自 S. cerevisiae 2 微米酵母质粒的复制源组成。 用上述载体转化酵母菌，特别是克鲁酵母属和酵母属的酵母菌后，被转化的酵母菌能更有效地产生外来蛋白质。 就茶黄素而言，信号多肽（前部分）的存在似乎是在酵母中表达所必需的。此外，还介绍了编码其他信号多肽的 DNA 序列。此外，还介绍了酵母在结构基因（最好是那些编码类thaumatin 蛋白和类糜蛋白酶蛋白的基因）和编码信号多肽的 DNA 序列中优先使用的密码子。
• Bicyclic AZA compounds as muscarinic M1 receptor and/or M4 receptor
  申请人：Heptares Therapeutics Limited

  公开号：US10961225B2

  公开（公告）日：2021-03-30

  This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.

  本发明涉及的化合物是毒蕈碱 M1 受体和/或 M4 受体的激动剂，可用于治疗毒蕈碱 M1/M4 受体介导的疾病。本发明还提供了含有这些化合物的药物组合物以及这些化合物的治疗用途。化合物包括根据式 1 的化合物或其盐，其中 Q、R1、R2、R3 和 R4 如本文所定义。