摘要
研究了3条合成法可林中间体[7,8-二氨基吩嗪-2-磺酸(1)]的工艺路线(路线A^C)。结果表明:路线C为最优反应条件,即以邻苯二胺为起始原料,先用浓硫酸磺化,再经保护-氧化反应,最后脱除保护基合成了1,总收率62.01%,其结构经~1H NMR,^(13)C NMR和ESI-MS确证。
Three routes( route A ~ C) of synthesizing phacolysin intermediate,7,8-diaminophenazine-2-sulfonic acid( 1),were investigated. The results showed that route C was the best method. 1 was synthesized by sulfuric acid sulfonation,protection-oxidation and deprotection,respectively. The total yield was 62. 01%. The structure was confirmed by^1 H NMR,^(13)C NMR and ESI-MS.
出处
《合成化学》
CAS
CSCD
2016年第5期461-463,468,共4页
Chinese Journal of Synthetic Chemistry
关键词
法可林
中间体合成
7
8-二氨基吩嗪-2-磺酸
药物合成
工艺优化
phacolysin
intermediate synthesis
7
8-diaminophenazine-2-sulfoniacid acid
drug synthesis
process improvement