反应详情

A mixture of 3-Amino-1-(8-methoxy-5,6-dihydro-benzo[h]quinazolin-2-yl)-1H-pyrazole-4-carboxylic acid (40 mg, 0.118 mM), diisopropylethylamine (70 ul, 0.402 mM), 4-[2-(4-Methyl-piperazin-1-yl)-ethyl]-phenylamine (30 mg, 0.1369 mM) in DMF (1 ml) to which was added HBTU (60 mg, 0.1583 mM) and the stirred 16 hr at room temperature. The resulting suspension was filtered and the solid washed with water (1×1 ml) and dried in vacuo to afford 5-Amino-1-(7-methoxy-5,6-dihydro-benzo[h]quinazolin-2-yl)-1H-pyrazole-4-carboxylic acid {4-[2-(4-methyl-piperazin-1-yl)-ethyl]-phenyl}-amide (12 mg, 19% yield) as a white solid. ES-MS MH+ 539. The filtrate may be purified via RP-HPLC 0.1% TFA to afford additional material.

1. customthe stirred 16 hr
2. customat room temperature
3. filtrationThe resulting suspension was filtered
4. washthe solid washed with water (1×1 ml)
5. customdried in vacuo