NEW MATERIAL:A fluorine-containing 2-butenolide derivative shown by formula I (n is 0-2; R1 and R2 are H or protecting group).
EXAMPLE: A compound wherein n in formula I is 0 and both R1 and R2 are t-butyldimethylsilyl.
USE: An intermediate for anti-cancer drug and antimicrobial agents. Having optical activity.
PREPARATION: A furan shown by formula III is reacted with n-BuLi and a compound shown by formula R1Cl in a solvent such as tetrahydrofuran and then reacted with n-BuLi and a compound shown by formula IV to form a compound shown by formula II, which is then reduced with a reducing agent such as NaBH4 in a solvent such as ethanol, then with acetyl chloride and further asymmetrically hydrolyzed with esterase to give compounds shown by formula V and formula VI. The compound shown by formula V is reacted with R2Cl, oxidized with an oxidizing agent such as magnesium monoperoxyphthalate and further with D-camphorsulfoniic acid to give a compound shown by formula I.
NAKAMURA KOICHI
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