Purine derivative with a cyclopropane ring, Process for Preparation and Method for preparing a purine derivative by cleavage of the cyclopropane unanillo from same

摘要

A purine derivative with a cyclopropane Ring represented by the formula (i) where a is a group or a - CH2 - Group Co - X1 is a hydrogen Atom, a Halogen Atom,An alkoxy Group of between 1 and 10 carbon Atoms or a hydroxyl Group, X2, X3 and X4 are each independently a hydrogen Atom or unu00e1tomo, halogen, R1 is a hydrogen Atom,A Halogen Atom or an amino Group protected or not protected, and R2 and R3 are each independently a hydrogen Atom,An alkyl group substituted or non substituted with 1 to 7 carbon ATOMS,A Group aralquilo replaced or nosustituido 7 to 11 Carbon Atoms or an acyl Group replaced or not replaced from 1 to 7 carbon ATOMS,With the condition that, in case that a is a co - or an acyl Group R2 nir3 are replaced or not replaced from 1 to 7 carbon Atoms and X3 and X4 are eachAn Atom dehalogeno regardless.A procedure for preparing a purine derivative which has a cyclopropane Ring represented by the formula (ii) wherein X1 is a hydrogen Atom, a Halogen Atom,An alkoxy Group of between 1 to 10 carbon ATOMS, or a hydroxyl Group, X2 is a hydrogen Atom or a Halogen Atom, X13 yx14 each independently is a Halogen Atom,R1 is a hydrogen Atom or a Halogen atom of an amino Group protected or not protected yr4 and R5 are each independently a hydrogen Atom,Alkyl group or a substituted nosustituido 1 to 7 carbon Atoms or a Group aralquilosustituido or not replaced from 7 to 11 u00e1toos carbonSaid method includes reacting a malonic acid derivative represented by laformula (V): where X7, X13 and x14 each independently.A Halogen Atom and R4 and R5 have the same meaning as above, with purine Compound represented by the formula (i) wherein X1,.R1 x2 and have the same meaning as above.A procedimientopara prepare underivado has a purine Ring cyclopropane (IIIA) represented by the formula: wherein X1 is a Halogen Atom, an alkoxy Group of 1 to 10 Atoms