Patent ID: 6486322
Filing Date: 2002-11-26
Classification: A61P,C07D

Abstract:
A process for preparing a compound of formula (II): whereinR is: a halogen atom or selected from the group consisting of â€”CN, â€”OH, â€”OCOR4, â€”(CH2)nNH2, â€”(CH2)nNHR4, â€”(CH2)nNHCOR4, â€”(CH2)nNHCONR4R5, â€”(CH2)nNHCOOR4, and â€”(CH2)nNHSO2R4, wherein n is either 0 or 1, and wherein R4 and R5 are, independently from each other, hydrogen or an optionally substituted group selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl, aryl, arylalkyl, arylalkenyl, arylalkynyl or, taken together to the nitrogen atom to which they are bonded, form an optionally substituted heterocyclyl group; and wherein R1 is optionally substituted alkyl, comprising: reacting a compound of formula (VII): â€ƒwith a) methylmagnesium iodide, thus obtaining a compound of formula (VIII): â€ƒand b) reacting the compound of formula (VIII) with a compound of formula (IX): R1COClâ€ƒâ€ƒ(IX) â€ƒwherein R1 is an optionally substituted alkyl group, thus obtaining a compound of formula (X): wherein R and R1 are as defined above; and c) hydrolyzing the compound of formula (X) in the presence of a base.