(2S,4S)-4-(4-methoxybenzylthio)-2-[(3S)-3-methylpiperazin-1-ylcarbonyl]-1-(4-nitrobenzyloxycarbonyl)pyrrolidine hydrochloride → (2S,4S)-4-(4-Methoxybenzylthio)-2-[(3S)-4-(N-4-nitrobenzyloxycarbonylacetimidoyl)-3-methylpiperazin-1-ylcarbonyl]-1-(4-nitrobenzyloxycarbonyl)pyrrolidine

HRID 727625ノート

反応式

HRID 727625 の反応式
Cl.[CH3:2][O:3][C:4]1[CH:38]=[CH:37][C:7]([CH2:8][S:9][C@@H:10]2[CH2:14][N:13]([C:15]([O:17][CH2:18][C:19]3[CH:24]=[CH:23][C:22]([N+:25]([O-:27])=[O:26])=[CH:21][CH:20]=3)=[O:16])[C@H:12]([C:28]([N:30]3[CH2:35][CH2:34][NH:33][C@@H:32]([CH3:36])[CH2:31]3)=[O:29])[CH2:11]2)=[CH:6][CH:5]=1.[N+:39]([C:42]1[CH:55]=[CH:54][C:45]([CH2:46][O:47][C:48]([NH:50][C:51](=N)[CH3:52])=[O:49])=[CH:44][CH:43]=1)([O-:41])=[O:40]>C(#N)C>[CH3:2][O:3][C:4]1[CH:5]=[CH:6][C:7]([CH2:8][S:9][C@@H:10]2[CH2:14][N:13]([C:15]([O:17][CH2:18][C:19]3[CH:20]=[CH:21][C:22]([N+:25]([O-:27])=[O:26])=[CH:23][CH:24]=3)=[O:16])[C@H:12]([C:28]([N:30]3[CH2:35][CH2:34][N:33]([C:51](=[N:50][C:48]([O:47][CH2:46][C:45]4[CH:54]=[CH:55][C:42]([N+:39]([O-:41])=[O:40])=[CH:43][CH:44]=4)=[O:49])[CH3:52])[C@@H:32]([CH3:36])[CH2:31]3)=[O:29])[CH2:11]2)=[CH:37][CH:38]=1

参加物

4

反応物 2

HCID 67585387(2S,4S)-4-(4-methoxybenzylthio)-2-[(3S)-3-methylpiperazin-1-ylcarbonyl]-1-(4-nitrobenzyloxycarbonyl)pyrrolidine hydrochlorideHCID 140352007HCID 140352007、化合物

生成物 1

HCID 88299347(2S,4S)-4-(4-Methoxybenzylthio)-2-[(3S)-4-(N-4-nitrobenzyloxycarbonylacetimidoyl)-3-methylpiperazin-1-ylcarbonyl]-1-(4-nitrobenzyloxycarbonyl)pyrrolidine収率 30.8%

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

実験手順

2.26 g of (2S,4S)-4-(4-methoxybenzylthio)-2-[(3S)-3-methylpiperazin-1-ylcarbonyl]-1-(4-nitrobenzyloxycarbonyl)pyrrolidine hydrochloride [prepared as described in step (i) above] were mixed with 1.14 g of N-(4-nitrobenzyloxycarbonyl)acetamidine and 45 ml of acetonitrile, and the mixture was heated under reflux for 16 hours. At the end of this time, the reaction mixture was worked up and purified by the same procedure as described in Preparation 1(ii), to give 922 mg of the title compound, as a powder.

後処理

  1. temperaturethe mixture was heated
  2. temperatureunder reflux for 16 hours
  3. custompurified by the same procedure
  4. customas described in Preparation 1(ii)

出典と根拠

ORDレコード
ord-eaf7e7548b7b4b85a6ebd8f2bef5f431
出典データセット
uspto-grants-1998_01
特許番号
US05712267

反応ノート

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