Interquim, S.a.

Healthtech Bio Actives, S.l.u.

Juan Sallares Rosell

Francisco Marquillas Olondriz

Francisco Marquillas

The present invention relates to a process for the purification of methylcobalamin, namely from iron cyanide impurities, comprising contacting a solution comprising methylcobalamin and iron cyanide anions with a strongly basic anion exchange resin. This purification process can advantageously be used for removing iron cyanide impurities from methylcobalamin obtained by reductive methylation of cyanocobalamin and wherein iron (II) salts are used as cyanide scavengers, thus providing methylcobalamin with a reduced iron content. Methylcobalamin (R is methyl). 

Process for the purification of methylcobalamin

The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABAreceptor. In this process, N-(5-acetyl-2-fluorophenyl)-N-methyl-acetamide (VI) is reacted with an excess of N,N-dimethylformamide dimethyl acetal (NNDMF-DMA). The present invention also provides a new process for the preparation of a compound with affinity for GABAreceptor, N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methyl-acetamide (II), which comprises the following steps: a) methylation of N-(5-acetyl-2-fluorophenyl)-N-acetamide (IV) with a methyl sulfonate, b) reaction of the resulting compound (VI) with NNDMF-DMA, and c) reaction of the resulting compound (I) with (5-amino-1H-pirazol-4-yl)thiophen-2-yl-methanone (III) in glacial acetic acid. The present invention also relates to new intermediate (VI). 

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Sant Cugat del Vallès, Spain

Juan Sallares Rosell