阿达帕林
产量(工程)
硫酸二甲酯
化学
试剂
再结晶(地质)
甲苯
组合化学
有机化学
催化作用
材料科学
古生物学
过氧化苯甲酰
冶金
聚合
生物
聚合物
作者
Zhichang Liu,Jiannan Xiang
摘要
Strategies that were adopted during the process development of adapalene to achieve a cost-effective commercial-scale synthesis are described herein. These included (1) the use of AcOH/H2SO4 to afford 2-(1-adamantyl)-4-bromophenol in quantitative yield; (2) the dimethyl sulfate methylation to enhance the yield of methylation to 95%; (3) direct conversion of the Grignard reagent into methyl 6-(3-(1-adamantyl)-4-methoxyphenyl)-2-naphthoate by the catalysis of both PdCl2(PPh3)2 and ZnCl2 in high yield; (4) the use of EDTA-disodium salt dihydrate to ensure the heavy metal's content within acceptable limits; (5) the use of toluene to simplify the original chromatographic purification to recrystallization. The pilot-scale synthesis of adapalene is described in detail in the Experimental Section.
科研通智能强力驱动
Strongly Powered by AbleSci AI