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

반응식

HRID 629706 반응식
[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

참가 물질

4

반응물 1

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

생성물 1

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

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 64092,2,2-Trifluoroethanol용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-89f2c3218b814a1681e58a1876a17109
출처 데이터셋
uspto-grants-2016_04
특허 번호
US09315475B2

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