Patent ID: 6342603
Filing Date: 2002-01-29
Classification: C07D

Abstract:
A process for preparing a cyclopropane ring-cleaved purine derivative represented by the formula (X): wherein A is a â€”CH2â€” group or â€”COâ€” group; X10 is a hydrogen atom, an alkoxy group having 1 to 10 carbon atoms, or hydroxyl group; and each of R2 and R3 is independently a hydrogen atom, an alkyl group having 1 to 7 carbon atoms, which may have a substituent, an aralkyl group having 7 to 11 carbon atoms, which may have a substituent, or an acyl group represented by the formula RC(O)â€” wherein R is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, which may have a substituent; and R10 is a hydrogen atom or a protected or unprotected amino group, with proviso that in a case where A is a â€”COâ€” group, neither R2 nor R3 is an acyl group, said substituent being selected from the group consisting of an alkoxy group having 1 to 6 carbon atoms, a hydroxy group, a nitro group, an amino group, a halogen atom, and a cyano group,comprising hydrogenating a purine derivative having a cyclopropane ring represented by the formula (I): â€ƒwherein X1 is a hydrogen atom, a halogen atom, an alkoxy group having 1 to 10 carbon atoms, or hydroxyl group; each of X2, X3, and X4 is independently a hydrogen atom or a halogen atom; R1 is a hydrogen atom, a halogen atom, or a protected or unprotected amino group; and A, R2 and R3 the same as defined above, with proviso that in a case where A is a â€”COâ€” group, neither R2 nor R3 is an acyl group, said substituent being selected from the group consisting if an alkoxy group having 1 to 6 carbon atoms, a hydroxy group, a nitro group, an amino group, a halogen atom, and a cyano group.