摘要
他达那非为口服磷酸二酯酶5(PDE 5)抑制剂,用于治疗男性勃起功能障碍(MED)。笔者以D-色氨酸为原料,先甲酯化反应,生成的D-色氨酸甲酯盐酸盐在异丙醇中与胡椒醛发生Pictet-spengler反应,得到顺式四氢咔啉化合物,然后再依次与氯乙酰氯和甲胺反应,总收率为56%,经过筛选,冰醋酸作为重结晶溶剂进行进一步纯化。
Tadalafil is a new phosphodiesterase 5 inhibitor used for the treatment of male erectile dysfunction(MED).For the preparation of tadalafil,D-tryptophan was used as the starting material.It was converted to its methyl ester,then underwent Pictet-spengler reaction with heliotropin in isopropanol to give the cis-tetrahydrocarboline,which was further reacted with chloroacetyl chloride,followed by methylamine.Tadalafil was obtained in an overall yield of 56% and was recrystallized from acetic acid.
出处
《精细化工中间体》
CAS
2010年第6期39-42,共4页
Fine Chemical Intermediates
