Patent ID: 6127539
Filing Date: 2000-10-03
Classification: C07D,C07F

Abstract:
A method for preparing a cyclopentenecarboxyamide derivative represented by the formula (I): ##STR23## wherein R.sup.1 is an electron withdrawing group having sulfur atom or phosphorus atom directly bonded to the nitrogen atom of the amido group, andY is a residue of a purine base, wherein said purine base may be substituted with one or more substituents selected from the group consisting of halogen, alkylamino, hydroxyl, alkoxy, alkylthio, amino and protected amino,comprising the steps of:(A) reacting in the presence of an organolithium compound and at a temperature of from -120.degree. C. to 0.degree. C., 2-azabicyclo[2.2.1]hept-5-en-3-one represented by the formula (IV): ##STR24## with a compound represented by the formula (V):R.sup.1 --X (V)wherein R.sup.1 is an electron withdrawing group having sulfur atom or phosphorus atom directly bonded to X, and X is a halogen atom, to yield a bicycloamide derivative represented by the formula (II): ##STR25## wherein R.sup.1 is defined as above; and (B) reacting the bicycloamide obtained in the step (A) in the presence of a base and a palladium catalyst with a compound represented by the formula (III):Y--H (III)wherein Y is as defined above.