ホームMCPワークベンチSkills
ホームワークベンチ通知マイページ
llms.txt · MCPガイドプライバシーポリシー · 利用規約 · サポートv1.8.0
  1. ホーム
  2. /反応

Ethanol → 3-[((2R,3R)-1-methyl-5-oxo-3-phenylpyrrolidin-2-yl)carbonyl](4S)-4-benzyl-1,3-oxazolidin-2-one

HRID 1837969
ノート
印刷プレビュー

反応式

HRID 1837969 の反応式
C[C:2]1([C:9]2[C@H:10]([C:14]([N:16]3[C@@H:20]([CH2:21][C:22]4[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=4)[CH2:19][O:18][C:17]3=[O:28])=[O:15])[NH:11][CH2:12]C=2)[CH2:7][C:6](=O)[CH:5]=[CH:4][CH2:3]1.CC1(C2[C@@H](C(N3[C@@H](CC4C=CC=CC=4)COC3=O)=O)NCC=2)CC(=O)C=CC1.[CH3:57][CH2:58][OH:59]>[Pd].CCOC(C)=O>[CH3:12][N:11]1[C:58](=[O:59])[CH2:57][C@H:9]([C:2]2[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=2)[C@@H:10]1[C:14]([N:16]1[C@@H:20]([CH2:21][C:22]2[CH:23]=[CH:24][CH:25]=[CH:26][CH:27]=2)[CH2:19][O:18][C:17]1=[O:28])=[O:15]
参加物実験手順後処理出典と根拠反応ノート

参加物

6

反応物 3

HCID 702EthanolHCID 69892003(4S)-3-[((2S)-1-methyl-5-oxo-3-phenyl(3-pyrrolin-2-yl))carbonyl]-4-benzyl-1,3-oxazolidin-2-oneHCID 86587927((2R)-1-methyl-5-oxo-3-phenyl(3-pyrrolin-2-yl)carbonyl](4S)-4-benzyl-1,3-oxazolidin-2-one

生成物 1

HCID 590664473-[((2R,3R)-1-methyl-5-oxo-3-phenylpyrrolidin-2-yl)carbonyl](4S)-4-benzyl-1,3-oxazolidin-2-one

試薬・触媒・溶媒 2

HCID 23938
Palladium
触媒
HCID 8857Ethyl Acetate溶媒

実験手順

To a slurry of 10% palladium on carbon (7.0 g) in EtOAc (700 mL) was added a solution of diastereomers 3-[((2R)-1-methyl-5-oxo-3-phenyl(3-pyrrolin-2-yl)carbonyl](4S)-4-benzyl-1,3-oxazolidin-2-one and (4S)-3-[((2S)-1-methyl-5-oxo-3-phenyl(3-pyrrolin-2-yl))carbonyl]-4-benzyl-1,3-oxazolidin-2-one (78.5 g, 0.208 mol) in EtOH (100 mL) and the reaction mixture was stirred under a H2 atmosphere (1 Atm) for 2 days. The reaction mixture was filtered through a pad of Celite® with the aid of EtOAc. The filtrate was concentrated under reduced pressure and purified by flash chromatography (gradient from 15% to 65% EtOAc/hex) to give diastereomer 3-[((2R,3R)-1-methyl-5-oxo-3-phenylpyrrolidin-2-yl)carbonyl](4S)-4-benzyl-1,3-oxazolidin-2-one as a single diastereomer (41.02 g, 52%): TLC (15% i-PrOH/hex) Rf0.25; 1H NMR (CDCl3) δ 1.39 (dd, J=11.4, 13.6 Hz, 1H), 2.45-2.51 (dd, J=3.3, 13.6 Hz, 1H), 2.87-2.91 (m, 5H), 3.91 (dd, J=9.2, 2.9 Hz, 1H), 4.03-4.23 (m, 3H), 4.36-4.43 (m, 1H), 5.75 (d, J=9.2 Hz, 1H), 7.01-7.03 (m, 2H), 7.21-7.39 (m, 8H); HPLC ES-MS m/z (rel abundance) 377 (MH+, 100%).

後処理

  1. filtrationThe reaction mixture was filtered through a pad of Celite® with the aid of EtOAc
  2. concentrationThe filtrate was concentrated under reduced pressure
  3. custompurified by flash chromatography (gradient from 15% to 65% EtOAc/hex)

出典と根拠

ORDレコード
ord-7576b0257cb34721ba1169e1cf0bb7fc
出典データセット
uspto-grants-2004_08
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US06784167B2

反応ノート

読み込み中…

このページの内容参加物実験手順後処理出典と根拠反応ノート