2-(naphthalen-1-yloxymethyl)-thiophene

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 2-(naphthalen-1-yloxymethyl)-thiophene
• 英文别名: 2-(Naphthalen-1-yloxymethyl)thiophene
• 化学式: C₁₅H₁₂OS
• mdl: MFCD20540974
• 分子量: 240.326
• InChiKey: RJYZOLZRGXQTAS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.066
• 拓扑面积：
  37.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(naphthalen-1-yloxymethyl)-thiophene 、 2-氯-N,N-二甲基乙胺 在 lithium diisopropyl amide 作用下， 以 四氢呋喃 为溶剂， 反应 14.5h， 生成 N,N-dimethylamino-3-(1-naphthanyloxy)-3-(2-thienyl)-1-propanamine
  参考文献：
  名称：

  A process for the preparation of aryloxypropylamines

  摘要：

  一种用于制备化合物（I）或其盐的方法，其中化合物可以是单个异构体或其混合物，其中A和B各自独立地是芳基或杂环芳基，可选择地取代1至4个取代基；而R和R1可以相同也可以不同，分别是氢、C1-C6烷基或氨基保护基；包括化合物（II）与化合物（III）的反应，其中A和B如上定义，R和R1各自独立地是C1-C6烷基或氨基保护基；X是一个离去基团；在碱性试剂的存在下进行；如果需要，将化合物（I）转化为另一种化合物（I）；如果需要，将化合物（I）的异构体混合物分离为单个异构体；如果需要，将化合物（I）转化为其盐。

  公开号：

  EP1857435A3

文献信息

• PROCESS FOR THE PREPARATION OF ARYLOXYPROPYLAMINES
  申请人：MANTEGAZZA Simone

  公开号：US20070270483A1

  公开（公告）日：2007-11-22

  A process for preparation of a compound of formula (I), or a salt thereof, both as individual isomer and as mixtures thereof, wherein each of A and B is independently aryl or heteroaryl optionally substituted with 1 to 4 substituents; and R and R 1 , which can be the same or different, are hydrogen, C 1 -C 6 alkyl or an amino-protecting group; comprising the reaction of a compound (II) wherein A and B are as defined above, with a compound (III) wherein each of R and R 1 is independently C 1 -C 6 alkyl or an amino-protecting group; and X is a leaving group; in the presence of a basic agent; and, if desired the conversion of a compound (I) to another compound (I); and/or, if desired, the separation of an isomeric mixture of a compound (I) into the individual isomers; and/or, if desired, the conversion of a compound (I) to a salt thereof.

  一种制备化合物(I)或其盐的方法，该化合物可以是单体异构体，也可以是它们的混合物，其中A和B分别独立地是芳基或杂环芳基，可选择地取代1到4个取代基；R和R1可以相同也可以不同，是氢、C1-C6烷基或氨基保护基；包括将化合物(II)（其中A和B如上定义）与化合物(III)（其中R和R1分别独立地是C1-C6烷基或氨基保护基；X是一个离去基团）在碱性试剂存在下反应；如有需要，将化合物(I)转化为另一种化合物(I)；和/或如有需要，将化合物(I)的异构混合物分离成单体异构体；和/或如有需要，将化合物(I)转化为其盐。
• [EN] SYNTHESIS OF DULOXETINE AND/OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF<br/>[FR] SYNTHÈSE DE DULOXÉTINE ET/OU DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES DE CELLE-CI
  申请人：KRKA D D NOVO MESTO

  公开号：WO2011128370A1

  公开（公告）日：2011-10-20

  The invention describes an improved process for the synthesis of duloxetine and/or pharmaceutically acceptable salts thereof enabling preparation of duloxetine and/or pharmaceutically acceptable salts thereof with high chemical and enatiomeric purity. The process includes addition of an organic acid in the phase of formation of a duloxetine salt with an acid, preferably in the form of hydrochloride, and optionally in the phase of recrystallization of the formed duloxetine salt, wherein an organic acid is preferably selected from the group comprising formic acid, acetic acid, propanoic acid, butanoic acid or any mixtures thereof, more preferably acetic acid.

  本发明描述了一种改进的杜氯嗪合成过程及其药学上可接受的盐，使得可以高纯度地制备杜氯嗪及其药学上可接受的盐。该过程包括在形成杜氯嗪盐的阶段中添加有机酸，优选为盐酸形式，并且在所形成的杜氯嗪盐的再结晶阶段中也可以添加有机酸。所述有机酸优选从包括甲酸、乙酸、丙酸、丁酸或任何混合物的群组中选择，更优选为乙酸。
• EP2558455B1
  申请人：——

  公开号：EP2558455B1

  公开（公告）日：2017-08-09
• [EN] COMPOSITIONS AND METHODS RELATING TO INHIBITING SERINE HYRDOXYMETHYLTRANSFERASE 2 ACTIVITY<br/>[FR] COMPOSITIONS ET PROCÉDÉS RELATIFS À L'INHIBITION DE L'ACTIVITÉ SÉRINE HYDROXYMÉTHYLTRANSFÉRASE 2
  申请人：UNIV MICHIGAN

  公开号：WO2016085990A1

  公开（公告）日：2016-06-02

  The present invention relates to small molecule compounds capable of inhibiting serine hydroxylmethyltransferase 2 (SHMT2) activity, methods for the discovery of such compounds, and related research and therapeutic uses for such compounds. In particular, the present invention provides compounds capable of inhibiting SHMT2 activity, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with diseases and other pathophysiological states caused by or associated with aberrant SHMT2 activity (e.g., cancer).
• A process for the preparation of aryloxypropylamines
  申请人：Dipharma Francis S.r.l.

  公开号：EP1857435A3

  公开（公告）日：2008-05-07

  A process for the preparation of a compound of formula (I), or a salt thereof, both as the as individual isomer and as mixtures thereof, wherein each of A and B is independently aryl or heteroaryl optionally substituted with 1 to 4 substituents; and R and R1, which can be the same or different, are hydrogen, C1-C6 alkyl or an amino-protecting group; comprising the reaction of a compound (II) wherein A and B are as defined above, with a compound (III) wherein each of R and R1 is independently C1-C6 alkyl or an amino-protecting group; and X is a leaving group; in the presence of a basic agent; and, if desired the conversion of a compound (I) to another compound (I); and/or, if desired, the separation of an isomeric mixture of a compound (I) into the individual isomers; and/or, if desired, the conversion of a compound (I) to a salt thereof.

  一种用于制备化合物（I）或其盐的方法，其中化合物可以是单个异构体或其混合物，其中A和B各自独立地是芳基或杂环芳基，可选择地取代1至4个取代基；而R和R1可以相同也可以不同，分别是氢、C1-C6烷基或氨基保护基；包括化合物（II）与化合物（III）的反应，其中A和B如上定义，R和R1各自独立地是C1-C6烷基或氨基保护基；X是一个离去基团；在碱性试剂的存在下进行；如果需要，将化合物（I）转化为另一种化合物（I）；如果需要，将化合物（I）的异构体混合物分离为单个异构体；如果需要，将化合物（I）转化为其盐。