Patent ID: 8232395

Claim:
A process for obtaining a compound of formula Ia: where R1 is a hydrogen atom, —(C 1 -C 12 )-alkyl, —(C 6 -C 14 )-aryl, —(C 3 -C 8 )-cycloalkyl or a 4- to 15-membered Het ring, R2 and R3 are the same or different and are each independently a hydrogen atom, (C 1 -C 12 )-alkyl, —(C 6 -C 14 )-aryl where aryl is unsubstituted or mono-, di- or trisubstituted by —(C 1-6 )-alkyl, —(C 3 -C 8 )-cycloalkyl or a 4- to 15-membered Het ring, said process comprising the steps of: a) reacting a boronoindole of the formula IV in which R1 is as defined in formula Ia, R4 and R5 are the same or different and are each independently —OH, —O—(C 1 -C 12 )-alkyl, —O—(C 6 -C 14 )-aryl, —O—(C 3-8 )-cycloalkyl, —(C 1 -C 12 )-alkyl or —O-Het, where Het is a 4- to 15-membered Het ring, or R4 and R5, together with the boron atom to which they are bonded, form a ring having 4, 5, 6 or 7 carbon atoms in the ring and the ring may, instead of the particular carbon atoms, contain two oxygen atoms or two oxygen atoms and one nitrogen atom, P is a hydrogen atom or a nitrogen protecting group, with an aminopyrimidine of the formula V in which R2 and R3 are each as defined in formula Ia and X is halogen, —O—SO 2 —R2, or —O—C(O)—R2, and detaching any nitrogen protecting group present, or b) reacting a boronoindole of the formula IV with a pyrimidine of the formula VI in which X is as defined in formula V and Y is halogen, —O—SO 2 —R2, or —O—C(O)—R2 to give a compound of the formula VII in which R1 and P are each as defined in formula IV and Y is as defined in the compound of the formula VI, and then reacting the compound of the formula VII with an amine of the formula VIII in which R2 and R3 are each as defined in formula Ia to give a compound of the formula Ia and detaching any nitrogen protecting group present, or c) reacting the alkyne of the formula IX in which R1 is as defined in formula Ia with a pyrimidine of the formula (V) to give an alkyne of the formula X in which R1, R2 and R3 are each as defined in formula Ia, and converting the compound of the formula X to the compound of the formula Ia by ring closure, or d) either isolating the compound of the formula Ia prepared by processes a), b) or c) in free form or, in the case of the presence of acidic or basic groups, converting it to physiologically compatible salts.