| 摘要 |
This invention relates to a process for the preparation of a compound, its solvate and its salt of formula I: <IMAGE> where RCO is an acyl group and the R group contains a substituted or unsubstituted aromatic carbocyclic or aromatic heterocyclic ring; R1 and R2 are independently of one another the groups hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl or C4-C12 cycloalkyl alkyl, or jointly form a branched or linear C2-C8 polymethylene group or C2-C6 alkenylene, optionally substituted with a hetero atom; R3 is hydrogen, C1-C6 alkyl or phenyl, or R3 jointly with R1 forms a -(CH2)3- or -(CH2)4 group; R4 and R5 are independently of one another hydrogen, hydroxy, halogen, C1-C6 alkyl or aryl, provided that both R4 and R5 are not hydrogen at the same time; and p is a whole number from 1 to 4. These compounds are useful in the treatment of pain or hyponatraemic conditions. The process for its preparation comprises, e.g. reacting a compound of formula III or its solvate or salt: <IMAGE> in which R'1 and R'2 are R1, R2 as defined for formula I or a group or atom convertible into R1 and R2, with a compound of formula R'COOH or a reactive derivative thereof, where R' and R are as defined for formula I, or a group which can be converted into R.
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