摘要
目的合成罗苏伐他汀的关键中间体 4 (4 氟苯基 ) 6 异丙基 2 (N 甲基 N 甲磺酰胺基 )嘧啶 5 羧酸甲酯。方法以异丁酰乙酸甲酯为起始原料 ,经与对氟苯甲醛缩合、S 甲基异硫脲硫酸盐环合、高锰酸钾氧化 ,再经甲胺基、甲磺酰基取代合成目标化合物。结果 5步反应总收率为2 5 0 %。结论改进了合成路线 。
Aim Synthesis the key intermediate of rosuvastatin 4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyrimidine-5-carboxylate.Method Synthesized from methyl isobutyrylacetate by condensation with 4-fluorobenzaldehyde,cylization with S-methylisothiourea sulfate,oxygenation by potassium permanganate,and substitution by methylamine and methanesulfonyl chloride respectively.Result The total yield of five steps is 25.0%.Conclusion Improve the synthetic methods and it is available to the synthesis of rosuvastatin.
出处
《中国药物化学杂志》
CAS
CSCD
2004年第3期148-149,157,共3页
Chinese Journal of Medicinal Chemistry
