Diisopropylethylamine → ethyl (2S)-2-(2-{4-[(2S)-2-hydroxy-3-(2-methylbenzothiazol-5-yloxy)propyl]piperazinyl}acetylamino)-2-(4-fluorophenyl)acetate

HRID 2217174

反応式

HRID 2217174 の反応式
Cl[CH2:2][C:3]([NH:5][C@@H:6]([C:12]1[CH:17]=[CH:16][C:15]([F:18])=[CH:14][CH:13]=1)[C:7]([O:9][CH2:10][CH3:11])=[O:8])=[O:4].[CH3:19][C:20]1[S:21][C:22]2[CH:28]=[CH:27][C:26]([O:29][CH2:30][C@@H:31]([OH:39])[CH2:32][N:33]3[CH2:38][CH2:37][NH:36][CH2:35][CH2:34]3)=[CH:25][C:23]=2[N:24]=1.C(N(C(C)C)CC)(C)C>C(O)C>[OH:39][C@H:31]([CH2:30][O:29][C:26]1[CH:27]=[CH:28][C:22]2[S:21][C:20]([CH3:19])=[N:24][C:23]=2[CH:25]=1)[CH2:32][N:33]1[CH2:34][CH2:35][N:36]([CH2:2][C:3]([NH:5][C@@H:6]([C:12]2[CH:17]=[CH:16][C:15]([F:18])=[CH:14][CH:13]=2)[C:7]([O:9][CH2:10][CH3:11])=[O:8])=[O:4])[CH2:37][CH2:38]1

参加物

5

反応物 3

HCID 81531DiisopropylethylamineHCID 58595334(2S)-1-(2-methylbenzothiazol-5-yloxy)-3-piperazinylpropan-2-olHCID 58719661Ethyl (2S)-2-(2-chloroacetylamino)-2-(4-fluorophenyl)acetate

生成物 1

HCID 58719662ethyl (2S)-2-(2-{4-[(2S)-2-hydroxy-3-(2-methylbenzothiazol-5-yloxy)propyl]piperazinyl}acetylamino)-2-(4-fluorophenyl)acetate

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

Ethyl (2S)-2-(2-chloroacetylamino)-2-(4-fluorophenyl)acetate (400 mg, 1.46 mmol), (2S)-3-(2-methylbenzothiazol-5-yloxy)-1-piperazinylpropan-2-ol (560 mg, 1.46 mmol), and 1.26 ml diisopropylethylamine (7.3 mmol) was refluxed in ethanol for 24 hours. Solvent was removed under reduced pressure, and the residue purified by Prep TLC, to provide ethyl (2S)-2-(2-{4-[(2S)-2-hydroxy-3-(2-methylbenzothiazol-5-yloxy)propyl]piperazinyl}acetylamino)-2-(4-fluorophenyl)acetate.

後処理

  1. customSolvent was removed under reduced pressure
  2. customthe residue purified by Prep TLC

出典と根拠

ORDレコード
ord-cf8f612187a2441ca45db2e36e1b938e
出典データセット
uspto-grants-2008_08
特許番号
US07407960B2

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