Process

Details Process Process

C - Chemistry, Metallurgy

07

D

C07D 209/24 (2006.01) C07C 209/50 (2006.01) C07C 211/15 (2006.01) C07C 211/29 (2006.01) C07C 231/18 (2006.01) C07C 233/05 (2006.01)

Patent

CA 2056068

A process for the preparation of (2R)-methyl-4;4,4-tri- fluorobutylamine, or an acid addition salt thereof which comprises a) acylating an optically active amine with 2-methyl-4,4,4- trifluorobutanoic acid or a reactive derivative thereof to afford a butyramide; b) separating (R)-diastereomeric butyramide from (S)-diastereomeric butyramide; and c) converting the (R)-diastereomeric butyramide into the desired (2R)-methyl-4,4,4-trifluorobutylamine, or an acid addition salt thereof. The product may be acylating with a carboxylic acid of formula III Image wherein U is carboxy, or a reactive derivative thereof to afford (R)-4-[5-(N-[4,4,4-trifluoro-2-methylbutyl]carbamoyl)-1-methylindol-3-yl- methyl]-3-methoxy-N-o-tolylsulphonylbenzamide. The indole is useful as a leukotriene antagonist, for example in the treatment of asthma or allergic rhinitis.

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