氟伐他汀钠的合成

Synthesis of Fluvastatin Sodium

氟苯和氯乙酰氯经付-克酰化、与N-异丙基苯胺缩合后环合,得3-(4-氟苯基)-1-异丙基-1H-吲哚,再经Vilsmeier-Haack反应、与乙酰乙酸甲酯缩合、选择性还原后水解成盐得HMG CoA还原酶抑制剂类降血脂药氟伐他汀钠,总收率约26%。

Fluvastatin sodium, an antihypercholesterolemic HMG CoA reductase inhibitor, was synthesized from fluorobenzene by Friedel-Crafts acylation with chloroacetyl chloride, followed by condensation with N-isopropyl aniline and cyclization to give 3-（4-fluorophenyl）-1-isopropyl-lH-indole, which was subjected to Vilsmeier-Haack reaction, condensation with methyl acetoacetate, selective reduction, hydrolysis and salt formation with an overall yield of 26%.