VERFAHREN ZUR HERSTELLUNG VON 2-THIENYLAMIN- DERIVATEN

PCT No. PCT/FR98/00441 Sec. 371 Date Sep. 2, 1999 Sec. 102(e) Date Sep. 2, 1999 PCT Filed Mar. 5, 1998 PCT Pub. No. WO98/39322 PCT Pub. Date Sep. 11, 1998The present invention relates to a process for the preparation of 2-thienylethylamine derivatives of general formula: as well as their acid additi...

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Hauptverfasser: PREVIERO, ALDO, CASTRO, BERTRAND, DORMOY, JEAN-ROBERT
Format: Patent
Sprache:ger
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Zusammenfassung:PCT No. PCT/FR98/00441 Sec. 371 Date Sep. 2, 1999 Sec. 102(e) Date Sep. 2, 1999 PCT Filed Mar. 5, 1998 PCT Pub. No. WO98/39322 PCT Pub. Date Sep. 11, 1998The present invention relates to a process for the preparation of 2-thienylethylamine derivatives of general formula: as well as their acid addition salts, in which R represents a halogen atom and R1 represents a C1-C4 alkyl group, characterized in that a thienylglycidic derivative of general formula: in which M represents an alkali metal atom or a fraction of an alkaline-earth metal atom, is reacted with a phenylglycine ester, optionally in the form of a strong acid salt, of general formula: in which R and R1 have the same meaning as above, in the presence of an alkali metal borchydride of general formula: X-YIV in which X represents an alkali metal atom and Y represents a group of formula: -BH3CN or -BH(4-w)Zw in which Z represents a carboxylic acid residue and optionally in the presence of a C1-C4 carboxylic acid, which gives the desired compound in the form of a free base which can be treated, if necessary, with an acid in order to obtain an addition salt of this compound.