Reacción #51430

Ecuación de reacción

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)

→

1H-Indole-2,5-dicarboxylic acid bis-{[2-(2-propylamino-ethylcarbamoyl)-1H-indol-5-yl]-amide}

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrodeprotection of Boc group and purification by HPLC
2. 2
   Otrogave GL496564 (39.4 mg, 63%)

Procedimiento

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+).

Fuente