| 摘要 |
The present invention provides a multistep process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)-ethylamine intermediates of the general formula:- <IMAGE> (I) in which R1, in the 2-, 3-, 4- or 5-position, is a hydrogen or halogen atom, a nitro, amino, cyano or carboxyl group, a linear or branched alkyl or alkoxy radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, R2 is a hydrogen atom, a linear or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, when the aminoethyl radical is in the two position and the radical R1 is in the 4- or 5-position, the above intermediates can be converted into 4,5,6,7-tetrahydrothieno[3,2-c]pyridine derivatives according to a procedure set forth in U.S. Pat. No. 4,127,580. When the aminoethyl radical is in the 3-position and the radical R1 is in the 4- or 5-position, the above intermediates can be converted into 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives according to a procedure set forth in U.S. Pat. No. 4,127,580. Both sets of tetrahydrothieno pyridine final products possess anti-inflammatory, vasodilator and blood platelet aggregation inhibition activity. |
