Process for the preparation of pyrimidine compounds

Details Process for the preparation of pyrimidine compounds Process for the preparation of pyrimidine compounds

C - Chemistry, Metallurgy

07

D

C07D 239/42 (2006.01) C07D 239/22 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2509344

A process for the preparation of a compound of Formula (I) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1-CO-CH2-E with a compound of formula R2-CHX1X2 in the presence of a compound of formula R3R4N-C(=NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (I). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent =O.

Cette invention concerne un procédé de préparation d'un composé représenté par la formule (I) et d'intermédiaires utiles. Ce procédé consiste à: faire réagir un composé de formule R?1¿-CO-CH¿2?-E avec un composé de formule R?2¿-CHX?1¿X?2¿ en présence d'un composé de formule R?3¿R?4¿N-C(=NH)NH¿2? et d'un catalyseur pour former une dihydropyrimidine; et à oxyder la dihydropyrimidine pour former le composé de formule (1).Dans cette formule, R?1¿ est H ou un groupe alkyle; R?2¿ est H, un alkyle ou un groupe aryle; R?3¿ et R?4¿ sont chacun indépendamment H, alkyle ou aryle, ou R?3¿ et R?4¿ sont reliés pour former, conjointement avec l'azote auquel ils sont liés, un noyau hétérocyclique comptant 5 à 7 membres; E est H, un groupe alkyle non substitué, un groupe aryle ou un groupe suppresseur d'électrons; et X?1¿ et X?2¿ sont chacun des groupes partants indépendamment, ou bien X?1¿ et X?2¿ ensemble =O.

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