5-Nitro-2-pyrrolidin-1-ylmethylbenzoxazole → 2-[(Pyrrolidin-1-yl)methyl]-1,3-benzoxazol-5-amine

HRID 2400363노트

반응식

HRID 2400363 반응식
[N+:1]([C:4]1[CH:5]=[CH:6][C:7]2[O:11][C:10]([CH2:12][N:13]3[CH2:17][CH2:16][CH2:15][CH2:14]3)=[N:9][C:8]=2[CH:18]=1)([O-])=O>[Pd].CCOC(C)=O.CO>[NH2:1][C:4]1[CH:5]=[CH:6][C:7]2[O:11][C:10]([CH2:12][N:13]3[CH2:14][CH2:15][CH2:16][CH2:17]3)=[N:9][C:8]=2[CH:18]=1

참가 물질

4

반응물 1

HCID 597669925-Nitro-2-pyrrolidin-1-ylmethylbenzoxazole

생성물 1

HCID 597669972-[(Pyrrolidin-1-yl)methyl]-1,3-benzoxazol-5-amine수율 100%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 21584119Ethylacetate methanol용매

실험 절차

To a solution of 5-nitro-2-[(pyrrolidin-1-yl)methyl]benzoxazole (300 mg, 1.21 mmol) in a mixed solvent of EtOAc-MeOH (1:1, 70 mL) was added 10% Pd—C (40 mg), the flask was purged with argon, then the argon was replaced with H2, the reaction mixture was stirred under H2 atmosphere for 30 min. After filtration through Celite, washed with ethyl acetate. The solvents were evaporated to provide 263 mg (100%) of 5-amino-2-[(pyrrolidin-1-yl)methyl]benzoxazole as a yellow solid.

후처리

  1. customthe flask was purged with argon
  2. filtrationAfter filtration through Celite
  3. washwashed with ethyl acetate
  4. customThe solvents were evaporated

출처 및 근거

ORD 기록
ord-0520fc1cf16541708cae4208b71cde02
출처 데이터셋
uspto-grants-2014_08
특허 번호
US08796259B2

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