反応 #51430
ord-8434c250265743c8ae7d86aa39a8ee78
反応方程式
Compound 82
(2-{[1-(5-Nitro-1H-indol-2-yl)-methanoyl]-amino}-ethyl)-propyl-carbamic acid dimethyl-ethyl ester
76
1H-Indole-2,5-dicarboxylic acid bis-{[2-(2-ethylamino-ethylcarbamoyl)-1H-indol-5-yl]-amide}
1H-indole-2,5-dicarboxylic acid bis-(pentafluorophenyl-amide)
1H-Indole-2,5-dicarboxylic acid bis-(pentafluorophenyl-amide)
→
反応物
Compound 82
(2-{[1-(5-Nitro-1H-indol-2-yl)-methanoyl]-amino}-ethyl)-propyl-carbamic acid dimethyl-ethyl ester
—
compound 83
76
1H-Indole-2,5-dicarboxylic acid bis-{[2-(2-ethylamino-ethylcarbamoyl)-1H-indol-5-yl]-amide}
1H-indole-2,5-dicarboxylic acid bis-(pentafluorophenyl-amide)
1H-Indole-2,5-dicarboxylic acid bis-(pentafluorophenyl-amide)
試薬
なし
反応条件
詳細条件
See reaction.notes.procedure_details.
後処理
- 1その他deprotection of Boc group and purification by HPLC
- 2その他gave GL496564 (39.4 mg, 63%)
実験手順
Compound 82 (131.2 mg, 0.336 mmol) was reduced to 83 by hydrogenation according to general procedure A in example 10. Similar procedure as described for the preparation of 76 from condensation of compound 83 with 1H-indole-2,5-dicarboxylic acid bis-(pentafluorophenyl-amide) 74 (45 mg, 0.084 mmol) followed deprotection of Boc group and purification by HPLC gave GL496564 (39.4 mg, 63%). ESI MS: 690.31 (M+H+), 345.66 (M/2+H+).