3-[甲氧基(甲基)氨基]-1-(2-噻吩基)-1-丙酮 | 802269-27-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 3-[甲氧基(甲基)氨基]-1-(2-噻吩基)-1-丙酮
• 英文名称: 3-[methoxy(methyl)amino]-1-(2-thienyl)-1-propanone
• 英文别名: 3-methoxymethylamino-1-(2-thienyl)-1-propanone；3-[Methoxy(methyl)amino]-1-thiophen-2-ylpropan-1-one
• CAS: 802269-27-8
• 化学式: C₉H₁₃NO₂S
• 分子量: 199.274
• InChiKey: SVMIPUPOUYMCQV-UHFFFAOYSA-N

物化性质

• 沸点：
  302.7±48.0 °C(Predicted)
• 密度：
  1.148±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  57.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-[甲氧基(甲基)氨基]-1-(2-噻吩基)-1-丙酮 在 trans-RuCl₂((R)-2,2'-bis(di-3,5-xylylphosphino)-1,1'-binaphthyl)((R)-1,1-di(4-anisyl)-2-isopropyl-1,2-ethylenediamine) potassium tert-butylate 、 氢气 作用下， 以 甲醇 、 二甲基亚砜 为溶剂， 反应 32.0h， 生成 度洛西汀
  参考文献：
  名称：

  Process for preparing (S)-(+)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine by using an optically active methylhydroxylaminopropanol compound as intermediate

  摘要：

  公开号：

  EP2386549B1

文献信息

• PREPARATION OF (S)-(+)-N-METHYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL) PROPYLAMINE USING OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AS AN INTERMEDIATE
  申请人：Chen Bo-Fong

  公开号：US20100234619A1

  公开（公告）日：2010-09-16

  The present invention provides a (S)-methylhydroxylaminopropanol derivative as an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate.

  本发明提供了一种(S)-甲基羟胺丙醇衍生物，作为制备(S)-(+)-N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺的中间体。本发明还提供了一种以更高的产率和更低的成本制备(S)-(+)-N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺的方法，其中使用(S)-甲基羟胺丙醇衍生物作为中间体。
• METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF 3-METHYLAMINO-1-(2-THIENYL)PROPAN-1-OL
  申请人：Chen Bo-Fong

  公开号：US20090112000A1

  公开（公告）日：2009-04-30

  The present invention provides a methylhydroxylaminopropanol derivative and the methylhydroxylaminopropanol derivative of the present invention is used as an intermediate for preparation of 3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (+)-(S)—N-methyl-3-methyl-3-( 1 -naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing 3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the methylhydroxylaminopropanol derivative is used as an intermediate.

  本发明提供了一种甲基羟胺丙醇衍生物，该甲基羟胺丙醇衍生物用作制备3-甲氨基-1-(2-噻吩基)丙醇的中间体，而该中间体又是制备(+)-(S)-N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺草酸盐的中间体。本发明还提供了一种制备3-甲氨基-1-(2-噻吩基)丙醇的方法，该方法具有更高的收率和更低的成本，其中使用了甲基羟胺丙醇衍生物作为中间体。
• PROCESS FOR PREPARING N-METHYL-N-HYDROXYL-3-(1-NAPHTHYLOXY)-3-(2-THIENYL)PROPYLAMINE DERIVATIVE
  申请人：Chen Bo-Fong

  公开号：US20100234620A1

  公开（公告）日：2010-09-16

  The present invention provides a process for preparing a N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and low treatment cost, which includes the preparation of the N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound.

  本发明提供了制备N-甲基-N-羟基-3-(1-萘氧基)-3-(2-噻吩基)丙胺化合物的方法。本发明还提供了一种制备(S)-(+)-N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺的方法，其产率更高，处理成本更低，其中包括制备N-甲基-N-羟基-3-(1-萘氧基)-3-(2-噻吩基)丙胺化合物的步骤。
• OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(-2-THIENYL)PROPAN-1-OL
  申请人：CHEN Bo-Fong

  公开号：US20120190869A1

  公开（公告）日：2012-07-26

  The present invention provides an (S)-methylhydroxylaminopropanol compound and the (S)-methylhydroxylaminopropanol compound of the present invention is used as an intermediate for preparation of (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(+3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol compound is used as an intermediate.

  本发明提供了一种(S)-甲基羟胺丙醇化合物，本发明的(S)-甲基羟胺丙醇化合物用作(S)-(−)-3-甲氨基-1-(2-噻吩基)丙醇的制备中间体，该中间体用于制备(S)-(+)-N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙胺草酸盐。本发明还提供了一种制备(S)-(+)-3-甲氨基-1-(2-噻吩基)丙醇的方法，其具有更高的产量和更低的成本，其中使用(S)-甲基羟胺丙醇化合物作为中间体。
• OPTICALLY ACTIVE METHYLHYDROXYLAMINOPROPANOL DERIVATIVE AND ITS USE AS INTERMEDIATE FOR PREPARATION OF (S)-(-)-3-METHYLAMINO-1-(2-THIENYL)PROPAN-1-OL
  申请人：CHEN Bo-Fong

  公开号：US20090112001A1

  公开（公告）日：2009-04-30

  The present invention provides an (S)-methylhydroxylaminopropanol derivative and the (S)-methylhydroxylaminopropanol derivative of the present invention is used as an intermediate for preparation of (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(−)-3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol derivative is used as an intermediate.

  本发明提供了(S)-甲基羟胺丙醇衍生物，本发明的(S)-甲基羟胺丙醇衍生物用作制备(S)-(−)-3-甲氨基-1-(2-噻吩基)丙醇的中间体，该中间体用于制备(S)-(+)-N-甲基-3-甲基-3-(1-萘氧基)-3-(2-噻吩基)丙基胺草酸盐。本发明还提供了一种制备(S)-(−)-3-甲氨基-1-(2-噻吩基)丙醇的方法，该方法具有更高的产率和更低的成本，其中使用(S)-甲基羟胺丙醇衍生物作为中间体。