| 摘要 |
This invention relates to a process for the preparation of a product of formula (I), wherein R is loweralkyl; R1 is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; R2 is loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; or R1 and R2 taken together with the nitrogen atom to which they are attached form a group of formula (Ia), wherein Y is hydrogen or loweralkyl and Z is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; and m is 0, 1 or 2; or a pharmaceutically acceptable salt thereof; which process comprises: (a) contacting a compound of formula (II) as defined herein with fortified hydrogen bromide to afford a compound of formula (III) as defined herein; (b) contacting the reaction mixture containing a compound of formula (III) with either: (1) an isocyanate of formula R1NCO, or (2) with a compound of formula (IV) as defined to afford a compound of formula (V) as defined herein, and (c) contacting the reaction mixture containing the compound of formula (V) with an amine of the formula R1R2NH herein in the presence of a carboxylic acid of the formula R5COOH and forming and isolating the product of formula (I).
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