| 摘要 |
<p>NEW MATERIAL:A 1,3-dioxolene-2-one derivative shown by the formula I (R1 is H, lower alkyl, or aryl; X is halogen; R2 is H or links with R1 through carbon chain into cyclic form). EXAMPLE:4-Bromomethyl-5-phenyl-1,3-dioxolene-2-one. USE:A modifying agent for prodrug of medicine. Easily reacting with an carboxylic acid to form a corresponding ester type compound, etc. The ester type compound is relatively stable in an alkaline medium corresponding to intestinal juice and hydrolyzed readily in the presence of an enzyme in the organism to restore the original compound. PROCESS:A compound shown by the formula II is reacted with a halogenating agent (e.g., Cl, Br, N-bromophthalic acid imide, etc.) in a nonproton inert organic solvent (e.g., hydrocarbon, etc.) in the presence of a radical inducer or by irradiation of ultraviolet rays, to give the titled compound shown by the formula I.</p> |
