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|Title:||Process for the manufacture of pharmaceutically active compounds|
|Abstract:||The present invention further relates to a process for the manufacture of compound (I), ##STR00001## wherein X is --Br or --Cl.|
|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:||Sep 13, 2012|
|Claims:||1. A process for the manufacture of compound (I), ##STR00037## comprising the steps of: aa) reacting the compound of formula (II), ##STR00038## with the compound of formula (III), ##STR00039## in the presence of a catalyst, copper(I)iodide and a base, to produce the compound of formula (IV), ##STR00040## bb) reacting said compound of formula (IV) in the presence of aqueous alkali metal hydroxide at 50-90.degree. C. and under reduced pressure to produce the compound of formula (V), ##STR00041## and cc) reacting said compound of formula (V) in the presence of aqueous alkali metal hydroxide or a strong base to produce the compound of formula (I); wherein R.sup.1 and R.sup.2 are each independently a C1-C4 alkyl, and X is --Br or --Cl. |
2. The process according to claim 1, wherein X is --Br.
3. The process according to claim 1, wherein R.sup.1 and R.sup.2 are both methyl.
4. The process according to claim 2, wherein reaction step bb) is carried out under reduced pressure below 100 mbar.
5. The process according to claim 1, wherein the catalyst in step aa) is PdCl.sub.2(PPh.sub.3).sub.2 and the alkali metal hydroxide in step bb) is lithium- or sodium hydroxide.
6. The process according to claim 1, wherein the compound of formula (IV) is dissolved in a mixture of water and N-methylpyrrolidone, and is reacted in the presence of aqueous sodium hydroxide at about 75 to about 85.degree. C. and under reduced pressure for 15 to 20 hours to give directly the compound of formula (I) without the need to apply an aqueous work-up of the compound of formula (V).
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