| 摘要 |
A process for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents, of formula I <CHEM> wherein R i s NHC*H(COOR<1>)CH2CH2COOR<1> or OR<1>; each R<1> is H or the same or different carboxy protecting group; the configuration about the carbon atom designated * is L; n is 0 or 1; and A/ &cir& is an aryl group which may be substituted; or a salt thereof, which comprises a) reacting 2,4-diamino-6-hydroxypyrimidine with a haloaldehyde of formula II <CHEM> wherein Y is bromo, chloro or iodo; and A/ &cir& , R, R<1>, n and * areas defined above; and b) optionally salifying the reaction product from step a). |
