左旋甲状腺素钠合成工艺的改进

Improved synthesis of levothyroxine sodium

以L-酪氨酸为原料,六步法合成左旋甲状腺素钠。对左旋甲状腺素钠合成的关键步骤——偶联反应的催化剂进行了改进,考察了偶联反应催化剂用量、溶剂用量、反应温度、反应时间等因素对反应的影响。工艺经改进后,偶联收率达60.5%,比文献报道提高了18.5%,6步反应总收率为22.5%,比文献值提高了11.1%。

Levothyroxine sodium was synthesized from L-tyrosine as raw material by six-step reactions.The catalyst in the key step of coupling reaction was improved.Some factors of coupling reaction were analyzed including the effect of amount catalyst,solvent amount,reaction temperature and reaction time.Under the optimal reaction conditions,the yield of coupling reaction could reached up to 60.5%,which was about 18.5% higher than before,the total yield of levothyroxine sodium could reached up to 22.5%,which was about 11.1% higher than before.