| 摘要 |
<p>PURPOSE: A process for preparing sescandelin and analogue thereof AGI-7 is provided, thereby easily preparing sescandelin and AGI-7 having improved angiogenesis-inhibiting activity in higher yield. CONSTITUTION: A process for preparing sescandelin of the formula(1) and AGI-7 of the formula(2) comprises the steps of: (a) reacting a compound of the formula(3) in formic acid or acetic acid or aqueous formic acid to form a ring structure and remove benzyl group as a protecting group, thereby preparing AGI-7 of formula(2); (b) selectively oxidizing 3-methyl-4-formyl isocumarin as a side-product of the step (a) using a oxidizing agent to purify the AGI-7 of the formula(2); and reducing acetyl group at C4 site of AGI-7 of the formula(2) using a reducing agent, wherein R is benzyl; the oxidizing agent is selected from RuO4, Ag2O, NaClO2, CrO3, KMnO4 and O2; and the reducing agent is selected from Li, Na, LiH, BH3, LiBH4, NaBH4, KBH4, Zn(BH4)2, NaBH3CN, LiBHEt3, Bu2AlH, LiAlH4, Et3SiH and SmI2.</p> |
