Ammonium formate → 1-(3,4,5-trimethoxybenzoyl)-3-(2-(4-(1-(1H-imidazol-2-ylmethyl)-1H-benzimidazol-2-yl-amino)piperidin-1-yl)ethyl)-3-(3,4-difluorophenyl) pyrrolidine

HRID 323317

반응식

HRID 323317 반응식
[CH3:1][O:2][C:3]1[CH:4]=[C:5]([CH:52]=[C:53]([O:57][CH3:58])[C:54]=1[O:55][CH3:56])[C:6]([N:8]1[CH2:12][CH2:11][C:10]([CH2:21][CH2:22][N:23]2[CH2:28][CH2:27][CH:26]([NH:29][C:30]3[N:34]([CH2:35][C:36]4[N:37](CC5C=CC=CC=5)[CH:38]=[CH:39][N:40]=4)[C:33]4[CH:48]=[CH:49][CH:50]=[CH:51][C:32]=4[N:31]=3)[CH2:25][CH2:24]2)([C:13]2[CH:18]=[CH:17][C:16]([F:19])=[C:15]([F:20])[CH:14]=2)[CH2:9]1)=[O:7].C([O-])=O.[NH4+]>CO.[Pd]>[CH3:58][O:57][C:53]1[CH:52]=[C:5]([CH:4]=[C:3]([O:2][CH3:1])[C:54]=1[O:55][CH3:56])[C:6]([N:8]1[CH2:12][CH2:11][C:10]([CH2:21][CH2:22][N:23]2[CH2:28][CH2:27][CH:26]([NH:29][C:30]3[N:34]([CH2:35][C:36]4[NH:40][CH:39]=[CH:38][N:37]=4)[C:33]4[CH:48]=[CH:49][CH:50]=[CH:51][C:32]=4[N:31]=3)[CH2:25][CH2:24]2)([C:13]2[CH:18]=[CH:17][C:16]([F:19])=[C:15]([F:20])[CH:14]=2)[CH2:9]1)=[O:7]

참가 물질

5

반응물 2

HCID 2723923Ammonium formateHCID 699552591-(3,4,5-trimethoxybenzoyl)-3-(2-(4-(1-(1-benzyl-1H-imidazol-2-ylmethyl)-1H-benzimidazol-2-yl-amino)piperidin-1-yl)ethyl)-3-(3,4-difluorophenyl) pyrrolidine

생성물 1

HCID 206422831-(3,4,5-trimethoxybenzoyl)-3-(2-(4-(1-(1H-imidazol-2-ylmethyl)-1H-benzimidazol-2-yl-amino)piperidin-1-yl)ethyl)-3-(3,4-difluorophenyl) pyrrolidine

시약·촉매·용매 2

HCID 23938Palladium촉매HCID 887Methanol용매

실험 절차

Combine 1-(3,4,5-trimethoxybenzoyl)-3-(2-(4-(1-(1-benzyl-1H-imidazol-2-ylmethyl)-1H-benzimidazol-2-yl-amino)piperidin-1-yl)ethyl)-3-(3,4-difluorophenyl) pyrrolidine (5 mmol) and 10% palladium-on-carbon (1.5 g) in methanol (50 mL). Add anhydrous ammonium formate (25 mmol). Heat to reflux. After 18 hours, filter, rinse with dichloromethane, and evaporate the filtrate in vacuo to give the title compound.

후처리

  1. temperatureHeat to reflux
  2. filtrationfilter
  3. washrinse with dichloromethane
  4. customevaporate the filtrate in vacuo

출처 및 근거

ORD 기록
ord-87aa56e966bd4303b7547e00eb71c990
출처 데이터셋
uspto-grants-2001_04
특허 번호
US06211199B1

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