利拉萘酯的合成

Synthesis of Liranaftate

用5,6,7,8-四氢-2-萘酚与硫光气反应得到的硫代氯甲酸5,6,7,8-四氢-2-萘酯和2-甲氧基-6-甲胺基吡啶在异丙醇-水中于室温反应2h得到抗真菌药物利拉萘酯,总收率70%。

Liranaftate was synthesized from 5,6,7,8-tetrahydro-2-naphthol by reaction with CSCl2 to give O-5,6,7,8-tetrahydro-2-naphthyl thiochloroformate, which subjected to acylation with 2-methoxy-6-methylaminopyridine in isopro-panol-H2O for 2h at room temperature in an overall yield of 70%.