| 摘要 |
A process for the preparation of tetrahydrothieno[3,2-c]pyridine derivative s of general formula I: (see formula I) or their pharmaceutically acceptable salts, wherein the meaning of X is hydrogen, carboxyl, alkoxycarbonyl, aryloxycarbonyl, nitrile, or carbamoyl of formula (see formula VI) wherein R, and R2 can be individually or simultaneously hydrogen, alkyl or part of a heterocyclic structure; Z can be hydrogen, halogen, alkyl, aryl, aryloxy or alkoxy group comprising the steps of: (a) reducing the compound of formula II with suitable reducing agents to obtain compound of formula III, (see formulas II and III) (b) reacting the compound of formula III with formaldehyde or any chemical equivalent thereof to obtain compound of formula IV, (see formula IV) (c) rearranging the compound of formula IV to produce the compound of formula V, (see formula V) wherein Y is hydroxyl, alkanoyloxy, aroyloxy, carbamate or carbonate derivatives, and (d) reducing the compound of formula V to compound of formula I.
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