Patent ID: 6320049
Filing Date: 2001-11-20
Classification: C07D

Abstract:
A process for the preparation of a compound of Formula (I): ##STR58##comprises treating a dihydropyrimidinone of Formula (II): ##STR59##with a deprotonation agent; then contacting the treated dihydropyrimidinone with carbonyldiimidazole to form an acylimidazolide intermediate; and then contacting the acylimidazolide intermediate with an amine of Formula (III):H.sub.2 N--R (III)to form the compound of Formula (I); whereinR.sup.1, R.sup.5 and R.sup.6 are each independently selected from:1) hydrogen,2) halogen,3) C.sub.1-10 alkyl,4) C.sub.3-8 cycloalkyl,5) substituted C.sub.1-10 alkyl, wherein the substituents are independently selected from halogen, C.sub.1-6 alkoxy, halogen-substituted C.sub.1-6 alkoxy, C.sub.3-6 cycloalkyl, phenyl, and halogen-substituted phenyl,6) substituted C.sub.3-8 cycloalkyl, wherein the substituents are independently selected from halogen, C.sub.1-6 alkoxy, halogen-substituted C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halogen-substituted C.sub.1-6 alkyl, phenyl, and halogen-substituted phenyl,7) phenyl, and8) substituted phenyl, wherein the substituents are independently selected from halogen, C.sub.1-4 alkyl, halogen-substituted C.sub.1-4 alkyl, cyano, nitro, and C.sub.1-4 alkoxy; orR.sup.1 is C.sub.1 -C.sub.4 alkoxy and R.sup.5 and R.sup.6 are each as defined above; orR.sup.1 is as defined above and R.sup.5 and R.sup.6 together form a 3- to 7-membered saturated or unsaturated carbocyclic ring or a 4- to 7-membered saturated or unsaturated heterocyclic ring, the carbocyclic ring or heterocyclic ring optionally substituted with C.sub.1-6 alkyl, wherein the heterocylic ring contains from 1 to 3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;R.sup.2 is:1) hydrogen,2) hydroxy,3) C.sub.1-10 alkyl,4) halogen-substituted C.sub.1-10 alkyl,5) C.sub.1-6 alkoxy,6) halogen-substituted C.sub.1-6 alkoxy,7) C.sub.3-6 cycloalkyl, or8) substituted C.sub.3-6 cycloalkyl, wherein the substituents are independently selected from halogen, hydroxy, C.sub.1-6 alkyl, halogen-substituted C.sub.1-6 alkyl, and C.sub.1-6 alkoxy;R.sup.3 and R.sup.4 are each independently selected from hydrogen, C.sub.1-10 alkyl, and the group of Formula (IV): ##STR60##wherein each Y is independently selected from1) halogen,2) cyano,3) C.sub.1-6 alkoxy,4) nitro,5) C.sub.1-10 alkyl, and6) halogen-substituted C.sub.1-10 alkyl;r is an integer of from 0 to 5;R.sup.7 is selected from hydrogen and C.sub.1-10 alkyl; andR is selected from C.sub.1-40 hydrocarbyl and substituted C.sub.1-40 hydrocarbyl.