2-(3-Benzyloxypyridin-4-yl)-5-(trifluoromethyl)benzoxazole → 4-[5-(Trifluoromethyl)benzoxazole-2-yl]pyridin-3-ol

HRID 884909노트

반응식

HRID 884909 반응식
C([O:8][C:9]1[CH:10]=[N:11][CH:12]=[CH:13][C:14]=1[C:15]1[O:16][C:17]2[CH:23]=[CH:22][C:21]([C:24]([F:27])([F:26])[F:25])=[CH:20][C:18]=2[N:19]=1)C1C=CC=CC=1.[H][H]>[Pd].C(O)(=O)C>[F:26][C:24]([F:25])([F:27])[C:21]1[CH:22]=[CH:23][C:17]2[O:16][C:15]([C:14]3[CH:13]=[CH:12][N:11]=[CH:10][C:9]=3[OH:8])=[N:19][C:18]=2[CH:20]=1

참가 물질

5

반응물 2

HCID 668801132-(3-Benzyloxypyridin-4-yl)-5-(trifluoromethyl)benzoxazoleHCID 178418361HCID 178418361, 화합물

생성물 1

HCID 1363312684-[5-(Trifluoromethyl)benzoxazole-2-yl]pyridin-3-ol수율 96.9%

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 176Acetic Acid용매

실험 절차

A mixture of 4.69 g of 2-(3-benzyloxypyridin-4-yl)-5-(trifluoromethyl)benzoxazole, 1.0 g of 5% palladium on carbon and 70 ml of acetic acid was stirred under about one atmosphere of hydrogen at room temperature for nine hours. The reaction mixture was filtered through Celite™. The filtrate was concentrated under reduced pressure. The residue was subjected to silica gel column chromatography to give 3.44 g of 4-[5-(trifluoromethyl)benzoxazole-2-yl]pyridin-3-ol (hereinafter, referred to as “active compound 114”).

후처리

  1. filtrationThe reaction mixture was filtered through Celite™
  2. concentrationThe filtrate was concentrated under reduced pressure

출처 및 근거

ORD 기록
ord-506b408851074ae4990bbe7d6f196093
출처 데이터셋
uspto-grants-2012_08
특허 번호
US08242133B2

반응 노트

불러오는 중…