Novel processes for the production of useful intermediates

A process for the production of a compound of formula (I), wherein said compound of formula (I)

• or a pharmaceutically acceptable salt or ester thereof, wherein
• R and R1 are independently, alkyl or benzyl, which benzyl is optionally substituted by one, two or three substituents including —O-alkyl;
• alkyl or halogen;
• with the proviso that:
• if R is alkyl, R1 in formula (I) may also be hydrogen or silyl, and R1 in formula (II) may also be silyl;
• R2 is hydrogen or halogen;
• is converted into a compound of formula (D)
• by:
• a) converting said compound of formula (I) into a compound formula (A)
• in the presence of a mineral acid and an ethereal solvent at temperatures between room temperature (RT) and 60° C.;
• and
• b) further reacting said compound of formula (A) with a compound of formula (B)
• in the presence of diisopropyl azodicarboxylate (DIAD), ethyldiphenylphosphine (EtPPh2) and dimethylacetamide (DMA), to give a compound of formula (C)
• and
• c) said compound of formula (C) is further reacted in the presence of palladium (II) acetate (Pd(OAc)2), potassium acetate (KOAc), triphenylphosphine (Ph3P), tetrabutyl ammonium bromide (Bu4NBr) and acetonitrile (MeCN) to give the corresponding compound of formula (D)
• wherein
• R2 is defined in claim 1;
• R8 and R9 are independently alkyl or halogen;
• and
• R10 is 4-methyl-piperidin-1-ylmethyl or hydrogen.

A compound of general formula (I)

• wherein
• R and R1 are independently alkyl or benzyl, which benzyl is optionally substituted by —O-alkyl;
• alkyl or halogen;
• and
• R2 is hydrogen or halogen.