Synthesis of derivatives of ginkgolide C

摘要

The subject invention provides ginkgolide C derivatives compounds having the structure: wherein R is H or -A-Ar, where A is an alkyl group; and Ar is an aryl group, which may contain heteroatoms and may be unsubstituted or substituted by one to five substituents each selected from the group consisting of hydrogen, alkoxy, -CH₂CO₂R⁴, and -CH₂CONR⁵R⁶; where R⁴ is an alkyl group; and R⁵ and R⁶ are each, independently, hydrogen or a branched or unbranched alkyl group; wherein R¹ is H or -COR⁷, where R⁷ is alkyl, aryl or amino; wherein R² is present or absent, and when present is H, -COR⁸ or -CO-Z-R⁸; where R⁸ is alkyl, aryl or amino; and Z is oxygen; wherein R³ is present or absent, and when present is -COR⁹; where R⁹ is alkyl or aryl; wherein only one of R² or R³ is present in the compound; wherein only two of R, R¹, R² and R³ are H; and wherein each of a and b designates a single covalent bond which is present or absent, where bond a is present when R³ is absent and bond b is present when R² is absent; or an optically pure enantiomer of the compound. Additionally, the subject invention provides methods of inhibiting the activity of a glycine receptor using these compounds.