摘要
以酪胺为起始原料,采用醋酸铜参与的芳基硼酸与酚的O-芳基化反应来构建芳基-O-芳基骨架,经5步反应合成了T2AM,经6步反应合成了T3AM和T4AM,总收率分别为44.5%、32.6%和38.3%。本文前期以I2-KI、后期以ICl-NaOCH3逐步对酚进行碘代来实现合成目的。O-芳基化反应时,发现分子筛的含水量也显著影响实验结果,故采用高温煅烧去水处理的分子筛进行该反应。
Three thyronamines were synthesized from tyramine via a copper-promoted O-arylation of arylboronic acids with phenols as a key step. T2AM was prepared in a 5-step sequence with a total yield of 44.5% while T3AM and T4AM were prepared in a 6-step sequence with an over yield of 32.6% and 38.3% respectively. I2-KI was used at early stage and ICI-NaOCH3 was then employed for iodination purpose. It was found that even trace amount of water contained in molecule sieves can greatly affect the Oarylation, so the reaction was carried out by using calcined molecule sieves.
出处
《中国药物化学杂志》
CAS
CSCD
2007年第6期392-394,共3页
Chinese Journal of Medicinal Chemistry