Dichloromethane → Ramipril

HRID 2187112

反応式

HRID 2187112 の反応式
C(O)(=O)/C=C\C(O)=O.C([O:16][C:17]([C@H:19]1[N:23]([C:24](=[O:42])[C@@H:25]([NH:27][C@H:28]([C:37]([O:39][CH2:40][CH3:41])=[O:38])[CH2:29][CH2:30][C:31]2[CH:36]=[CH:35][CH:34]=[CH:33][CH:32]=2)[CH3:26])[C@H:22]2[CH2:43][CH2:44][CH2:45][C@H:21]2[CH2:20]1)=[O:18])C1C=CC=CC=1.ClCCl>C(N(CC)CC)C>[CH3:41][CH2:40][O:39][C:37]([C@@H:28]([NH:27][C@H:25]([C:24]([N:23]1[C@H:19]([C:17]([OH:18])=[O:16])[CH2:20][C@H:21]2[C@@H:22]1[CH2:43][CH2:44][CH2:45]2)=[O:42])[CH3:26])[CH2:29][CH2:30][C:31]1[CH:32]=[CH:33][CH:34]=[CH:35][CH:36]=1)=[O:38]

参加物

4

反応物 2

HCID 6344DichloromethaneHCID 10121882HCID 10121882、化合物

生成物 1

HCID 5362129Ramipril

試薬・触媒・溶媒 1

HCID 8471Triethylamine溶媒

反応条件

温度
2.5 °C

実験手順

A 1.0 g portion of (2S,3aS,6aS)-1-[(S)-2-[[(S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]propanoyl]octahydrocyclopenta[b]pyrrole-2-carboxylic acid benzyl ester maleic acid salt 1 was placed into 100 mL of dichloromethane, and was cooled to 0-5° C. Triethylamine (0.19 g) was added to the mixture. The resulting mixture was washed with water, and the organic phase was evaporated to give an oil. This oil was deprotected using hydrogenolysis, as per examples stated in EP 079022 to give Ramipril as a white solid.

後処理

  1. washThe resulting mixture was washed with water
  2. customthe organic phase was evaporated
  3. customto give an oil

出典と根拠

ORDレコード
ord-2ba52ce1ab474547a63de27377c6daf5
出典データセット
uspto-grants-2002_06
特許番号
US06407262B1

関連ノート

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