tert-butyl (2R,5S)-2-[(2-aminopyridin-3-yl)ethynyl]-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)morpholine-4-carboxylate → tert-butyl (2R,5S)-2-[2-(2-aminopyridin-3-yl)ethyl]-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)morpholine-4-carboxylate

HRID 629706

反応式

HRID 629706 の反応式
[NH2:1][C:2]1[C:7]([C:8]#[C:9][C@H:10]2[O:15][CH2:14][C@@H:13]([CH2:16][O:17][Si:18]([C:21]([CH3:24])([CH3:23])[CH3:22])([CH3:20])[CH3:19])[N:12]([C:25]([O:27][C:28]([CH3:31])([CH3:30])[CH3:29])=[O:26])[CH2:11]2)=[CH:6][CH:5]=[CH:4][N:3]=1>FC(F)(F)CO.[Pd]>[NH2:1][C:2]1[C:7]([CH2:8][CH2:9][C@H:10]2[O:15][CH2:14][C@@H:13]([CH2:16][O:17][Si:18]([C:21]([CH3:22])([CH3:23])[CH3:24])([CH3:19])[CH3:20])[N:12]([C:25]([O:27][C:28]([CH3:31])([CH3:30])[CH3:29])=[O:26])[CH2:11]2)=[CH:6][CH:5]=[CH:4][N:3]=1

参加物

4

反応物 1

HCID 86726311tert-butyl (2R,5S)-2-[(2-aminopyridin-3-yl)ethynyl]-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)morpholine-4-carboxylate

生成物 1

HCID 86726313tert-butyl (2R,5S)-2-[2-(2-aminopyridin-3-yl)ethyl]-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)morpholine-4-carboxylate

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 64092,2,2-Trifluoroethanol溶媒

実験手順

To tert-butyl (2R,5S)-2-[(2-aminopyridin-3-yl)ethynyl]-5-({[tert-butyl(dimethyl)silyl]oxy}methyl)morpholine-4-carboxylate (1 eq.) in 2,2,2,-trifluoroethanol (0.4 M) at rt was added 10% Pd/C (0.2 eq.). The reaction was degassed and then shaken under 1 atm of H2 for 24 hrs. The reaction mixture was filtered on celite and concentrated to afford the desired compound.

後処理

  1. customThe reaction was degassed
  2. filtrationThe reaction mixture was filtered on celite
  3. concentrationconcentrated

出典と根拠

ORDレコード
ord-89f2c3218b814a1681e58a1876a17109
出典データセット
uspto-grants-2016_04
特許番号
US09315475B2

関連ノート

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