反应详情

温度

0 °C

To a solution of (Z)-2-amino-α-[(1-carboxy-1-methylethoxy)imino]-4-thiazoleacetic acid, methyl ester (3.16 g, 11.0 mmol) in dimethylformamide (44 ml) and N,N-diisopropylethylamine (2.11 ml, 12.1 mmol) at -10° C. was added diphenylchlorophosphate (2.51 ml, 12.1 mmol). After one hour at -10° C., a solution of N-tritylpiperazine (3.87 g, 11.0 mmol correcting for 7% by weight triethylamine) in tetrahydrofuran (20 ml) and triethylamine (1.54 ml, 11.0 mmol) was added over 15 minutes. The reaction was stirred for an additional 15 minutes at -10° C. and for 2 hours at 0° C.