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

反応式

[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]

参加物

実験手順

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.

後処理

temperatureHeat to reflux
filtrationfilter
washrinse with dichloromethane
customevaporate the filtrate in vacuo

出典と根拠

ORDレコード: ord-87aa56e966bd4303b7547e00eb71c990
出典データセット: uspto-grants-2001_04
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US06211199B1

反応式

参加物

反応物 2

生成物 1

試薬・触媒・溶媒 2

実験手順

後処理

出典と根拠

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