| 摘要 |
A PROCESS FOR MAKING 1,3-DISUBSTITUTED-4-OXOCYCLIC UREAS OF THE GENERAL FORMULA :@( FORMULA I )@R1, R2, AND R3 ARE INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF NIL, C1,F,BR,NH2, NO2, COOH, CH3SO2NH, SO3H, OH, ALKOXY. ALKYL, ALKOXYCARBONYL, HYDROXYALKYL, AND ACYLOXY;@R4, IS SELEDTED FROM THE GROUP CONSISTING OF A SUBSTITUTED ALKYL, ALKENYL, ALKYNYL, ALKYLACYL, AND HETEROALKYL; AND @A IS A SUBSTITUTED OR UNSUBSTITUTED, SATURATED OR UNSATURATED, STRAIGHT-CHAIN OR BRANCHED ALKYL OR ALKENYL AMINO GROUP COMPRISED OF 1-7 CARBON ATOMS; OR A IS A SUBSTITUTED OR UNSUBSTITUTED, SATURATED OR UNSATURATED HETEROCYCLE HAVING 5,6, OR 7 MEMBERS CONTAINING AT LEAST ONE NITROGEN, AND R4 IS ATTACHED TO THIS NITROGEN; WHEREIN SAID 1,3-DISUBSTITUTED-4-OXOCYCLIC UREA IS MADE WITHOUT ISOLATION OF INTERMEDIATES AND COMPRISING THE STEPS:(IA)REACTING A 1-SUBSTITUTED-4-OXOCYCLIC UREA WITH A CARBON CHAIN CONTAINING AT LEAST TWO LEAVING GROUPS IN THE PRESENCE OF A MILD BASE AND A SOLVENT TO FORM AN ADDUCT CONTAINING AT LEAST ONE LEAVING GROUP, AND(IB)CONDENSING THE ADDUCT WITH AN AMINE TO FORM A 1,3-DISUBSTITUTED-4-OXOCYCLIC UREA, AND(II)RECOVERING SAID 1,3-DISUBSTITUTED-4-OXOCYCLIC UREA, ARE DISCLOSED. THIS METHOD IS PARTICULARLY PREFERRED FOR MAKING 1[[[5-(4-CHOLOROPPHENYL)-2-FURANYL]METHYLENE]AMINO]-3-[4-(4-METHYL-1- PIPERAZINYL)BUTYL)-2,4-IMIDAZOLIDINEDIONE.
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