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Details for Patent: 8,329,724

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Details for Patent: 8,329,724

Title:Process for the manufacture of pharmaceutically active compounds
Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 ##STR00001## as well as novel synthesis routes for key intermediates used in those processes.
Inventor(s): Hildbrand; Stefan (Gelterkinden, CH), Mair; Hans-Juergen (Loerrach, DE), Radinov; Roumen Nikolaev (West Caldwell, NJ), Ren; Yi (Shanghai, CN), Wright; James Anderson (Cedar Grove, NJ)
Assignee: Hoffmann-La Roche Inc. (Nutley, NJ)
Filing Date:Jul 27, 2010
Application Number:12/843,908
Claims:1. A process for the manufacture of the compound of formula (1), ##STR00037## comprising the steps of reacting the compound of formula (5), ##STR00038## with 4-chlorophenylboronic acid in the presence of a palladium Catalyst to produce the compound of formula (6), ##STR00039## and cleaving the 2,6-dichlorobenzamide group in said compound of formula (6) to produce the compound of formula (1).

2. The process according to claim 1, wherein the compound of formula (5) is obtained by: reacting the compound of formula (2), ##STR00040## with oxalylchloride to produce the corresponding acid chloride; reacting said acid chloride with 5-bromo-7-azaindole in the presence of aluminium trichloride to produce the compound of formula (4), ##STR00041## and reacting said compound of formula (4) with 2,6-dichlorobenzoylchloride to produce the compound of formula (5).

3. The process according to claim 1, wherein: (A) said compound of formula (5) is obtained by: reacting the compound of formula (2) ##STR00042## with oxalylchloride in the presence of methylenechloride and N,N-Dimethylformamide to produce the corresponding acid chloride; reacting said acid chloride with 5-bromo-7-azaindole in the presence of aluminium trichloride to produce the compound of formula (4) ##STR00043## and reacting said compound of formula (4) with dichlorobenzoylchloride in the presence of dimethylaminopyridine and n-tripropylamine to produce the compound of formula (5) ##STR00044## and (B) said cleavage of the 2,6-dichlorobenzamide group in said compound of formula (6) is accomplished by reacting said compound with ammonia in methanol or ethanol solution diluted with a polar aprotic solvent.
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