| 摘要 |
PURPOSE:To prepare the titled compound useful as a raw material for the partial synthesis of homoharringtonine, by condensing the Na salt of 2-keto-1,4- butanedioic acid diethyl ester with 1-bromo-3-methylbutene-(2) in the presence of a phase transfer catalyst, and decarboxylating the condensation product. CONSTITUTION:The compound of formulaIis condensed with the compound of formula II in the presence of a phase transfer catalyst (e.g. benzyl.triethyl. ammonium chloride) to obtain 2-ethoxyoxalyl-5-methyl-4-hexenoic acid ethyl ester of formula III, which is decarboxylated to obtain the objective compound of formula IV in high yield and purity. Homoharringtonine synthesized from the compound of formula IV exhibits the activity to suppress the abnormal proliferation of cell, and useful as a remedy for non-lymphatic leukemia. It has comparable antitumor activity to and stronger biological activity than harringtonine which is homologue of the compound. |
