Patent ID: 6833457
Filing Date: 2004-12-21
Classification: C07D,C07F,Y02P

Abstract:
A process for the preparation of a compound represented by the formula: whereinG1 is a bond, CO or SO2, R2 is a hydrogen atom, a hydrocarbon group optionally having substituents, an alkoxy group optionally having substituents or a heterocyclic group optionally having substituents, R4 is a hydrogen atom, a hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, an alkoxy group optionally having substituents, an aryloxy group optionally having substituents or an amino group optionally having substituents, and R5 is a cyclic hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, which comprises:reacting a compound represented by the formula: â€ƒwherein X1 is a halogen atom and X2 is a leaving group, with a compound represented by the formula: R2NH2â€ƒâ€ƒ(VII) â€ƒwherein R2 is as defined above, or a salt thereof, to give a compound represented by the formula: â€ƒwherein R2 and X1 are as defined above, or a salt thereof; reacting the compound represented by the formula (IV) or a salt thereof with a trialkyl phosphite represented by the formula: (R3O)3Pâ€ƒâ€ƒ(V) â€ƒwherein R3 is a lower alkyl group; thereafter reacting with a compound represented by the formula: â€ƒwherein R1 is a hydrogen atom or an amino-protecting group, or a salt thereof, to give a compound represented by the formula: â€ƒwherein R1 and R2 are as defined above, or a salt thereof; reducing and thereafter where necessary deprotecting the compound represented by the formula (III) or a salt thereof to give a compound represented by the formula: â€ƒwherein R2 is as defined above, or a salt thereof; and reacting the compound represented by the formula (VIIIâ€²) or a salt thereof with a compound represented by the formula: â€ƒwherein X3 is a leaving group and G1, R4 and R5 are as defined above, or a salt thereof.