Trifluoroacetic acid → 4-[6-(5-{3-Cyano-4-[(1-methylethyl)oxy]phenyl}-1,2,4-oxadiazol-3-yl)-5-methyl-1,2,3,4-tetrahydro-1-isoquinolinyl]butanoic acid trifluoroacetate

HRID 2383329ノート

反応式

HRID 2383329 の反応式
[F:1][C:2]([F:7])([F:6])[C:3]([OH:5])=[O:4].[C:8]([C:10]1[CH:11]=[C:12]([C:20]2[O:24][N:23]=[C:22]([C:25]3[C:26]([CH3:48])=[C:27]4[C:32](=[CH:33][CH:34]=3)[CH:31]([CH2:35][CH2:36][CH2:37][C:38]([OH:40])=[O:39])[N:30](C(OC(C)(C)C)=O)[CH2:29][CH2:28]4)[N:21]=2)[CH:13]=[CH:14][C:15]=1[O:16][CH:17]([CH3:19])[CH3:18])#[N:9]>ClCCl>[F:1][C:2]([F:7])([F:6])[C:3]([OH:5])=[O:4].[C:8]([C:10]1[CH:11]=[C:12]([C:20]2[O:24][N:23]=[C:22]([C:25]3[C:26]([CH3:48])=[C:27]4[C:32](=[CH:33][CH:34]=3)[CH:31]([CH2:35][CH2:36][CH2:37][C:38]([OH:40])=[O:39])[NH:30][CH2:29][CH2:28]4)[N:21]=2)[CH:13]=[CH:14][C:15]=1[O:16][CH:17]([CH3:19])[CH3:18])#[N:9]

参加物

4

反応物 2

HCID 6422Trifluoroacetic acidHCID 595910904-(6-(5-{3-Cyano-4-[(1-methylethyl)oxy]phenyl}-1,2,4-oxadiazol-3-yl)-2-{[(1,1-dimethylethyl)oxy]carbonyl}-5-methyl-1,2,3,4-tetrahydro-1-isoquinolinyl)butanoic acid

生成物 1

HCID 687752864-[6-(5-{3-Cyano-4-[(1-methylethyl)oxy]phenyl}-1,2,4-oxadiazol-3-yl)-5-methyl-1,2,3,4-tetrahydro-1-isoquinolinyl]butanoic acid trifluoroacetate収率 72.7%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

反応条件

温度
25 °C

実験手順

Trifluoroacetic acid (1.0 ml, 13.0 mmol) was added dropwise at 25° C. under nitrogen to a solution of 4-(6-(5-{3-cyano-4-[(1-methylethyl)oxy]phenyl}-1,2,4-oxadiazol-3-yl)-2-{[(1,1-dimethylethyl)oxy]carbonyl}-5-methyl-1,2,3,4-tetrahydro-1-isoquinolinyl)butanoic acid (Preparation 32; 102 mg, 0.182 mmol) in dichloromethane (4.0 ml) and the resulting mixture was stirred at 25° C. for 1 h. The solvent was removed, and the residue co-evaporated with toluene followed by trituration with diethyl ether to give the title compound (76 mg) as a white solid.

後処理

  1. customThe solvent was removed

出典と根拠

ORDレコード
ord-43875f3202054fb6a211ba3436cfef40
出典データセット
uspto-grants-2012_09
特許番号
US08263620B2

反応ノート

読み込み中…