Tert-butyl acetoacetate → (2S,4R)-1-(3-oxo-butyryl)-4-[4-(2,2,2-trifluoro-ethoxy)-2-trifluoromethyl-benzenesulfonyl]-pyrrolidine-2-carboxylic acid methyl ester

HRID 1697596

反応式

HRID 1697596 の反応式
[CH3:1][O:2][C:3]([C@@H:5]1[CH2:9][C@@H:8]([S:10]([C:13]2[CH:18]=[CH:17][C:16]([O:19][CH2:20][C:21]([F:24])([F:23])[F:22])=[CH:15][C:14]=2[C:25]([F:28])([F:27])[F:26])(=[O:12])=[O:11])[CH2:7][NH:6]1)=[O:4].COC([C@@H]1C[C@@H](S(C2C=CC(F)=CC=2C(F)(F)F)(=O)=O)CN1)=O.[C:52](OC(C)(C)C)(=[O:57])[CH2:53][C:54]([CH3:56])=[O:55].COC([C@@H]1C[C@@H](S(C2C=CC(F)=CC=2C(F)(F)F)(=O)=O)CN1C(=O)CC(=O)C)=O>>[CH3:1][O:2][C:3]([C@@H:5]1[CH2:9][C@@H:8]([S:10]([C:13]2[CH:18]=[CH:17][C:16]([O:19][CH2:20][C:21]([F:22])([F:23])[F:24])=[CH:15][C:14]=2[C:25]([F:26])([F:28])[F:27])(=[O:12])=[O:11])[CH2:7][N:6]1[C:52](=[O:57])[CH2:53][C:54](=[O:55])[CH3:56])=[O:4]

参加物

5

反応物 4

HCID 15538Tert-butyl acetoacetateHCID 66770389HCID 66770389、化合物HCID 86646828(2S,4R)-4-(4-Fluoro-2-trifluoromethyl-benzenesulfonyl)-1-(3-oxo-butyryl)-pyrrolidine-2-carboxylic Acid Methyl EsterHCID 86646838(2S,4R)-4-[4-(2,2,2-Trifluoro-ethoxy)-2-trifluoromethyl-benzenesulfonyl]-pyrrolidine-2-carboxylic Acid Methyl Ester

生成物 1

HCID 86646840(2S,4R)-1-(3-oxo-butyryl)-4-[4-(2,2,2-trifluoro-ethoxy)-2-trifluoromethyl-benzenesulfonyl]-pyrrolidine-2-carboxylic acid methyl ester

実験手順

In analogy to the procedure described in example 192f, (2S,4R)-4-[4-(2,2,2-trifluoro-ethoxy)-2-trifluoromethyl-benzenesulfonyl]-pyrrolidine-2-carboxylic acid methyl ester containing (2S,4R)-4-(4-fluoro-2-trifluoromethyl-benzenesulfonyl)-pyrrolidine-2-carboxylic acid methyl ester was reacted with tert-butyl acetoacetate to give a mixture of the title compound and (2S,4R)-4-(4-fluoro-2-trifluoromethyl-benzenesulfonyl)-1-(3-oxo-butyryl)-pyrrolidine-2-carboxylic acid methyl ester as colorless oil. MS (ESI): m/z=520.2 [M+H]+.

後処理

  1. customto give

出典と根拠

ORDレコード
ord-d9d0f16222914d1a859401d0b22fd9f0
出典データセット
uspto-grants-2012_04
特許番号
US08163793B2

関連ノート

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