羟基法舒地尔的合成

Synthesis of Hydroxyfasudil

异喹啉经过硼酸钠氧化得异喹啉氮氧化物,在乙酐中发生重排得到1-羟基异喹啉,再用氯磺酸氯磺化,最后与高哌嗪反应得到Rho激酶抑制剂羟基法舒地尔,总收率为10.3%。

Hydroxyfasudil, a Rho-kinase inhibitor, was synthesized from isoquinoline by oxidation with sodium perborate to give isoquinoline-N-oxide, which was subjected to the rearrangement in acetic anhydride to give 1-hydroxyisoquinoline, followed by chlorosulfonation and condensation with homopiperazine with an overall yield of 10.3 %.