Method for preparing 2-thienylethylamine derivatives

Patent 6080875 Issued on June 27, 2000. Estimated Expiration Date:

September 2, 2019. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Abstract Claims Description Full Text

Patent References

Process for the preparation of N-(2-chlorobenzyl)-2-(2-thienyl) ethylamine
Patent #: 4873343
Issued on: 10/10/1989
Inventor: Radisson

2-thienylglycidic derivative, process for its preparation and its use as synthesis intermediate
Patent #: 5132435
Issued on: 07/21/1992
Inventor: Bousquet, et al.

Process for the preparation of an n-phenylacetic derivative of tetrahydrothieno(3,2-c)pyridine and its chemical intermediate Patent #: 5204469
Issued on: 04/20/1993
Inventor: Descamps, et al.

Inventors

Assignee

Sanofi-Synthelabo

Application

No. 380450 filed on 09/02/1999

US Classes:

549/77Unsaturated carbocyclic ring or acyclic carbon to carbon unsaturation containing

Examiners

Primary: Lambkin, Deborah C.

Attorney, Agent or Firm

Alexander; Michael D.

Foreign Patent References

321349 EP. 06/13/1989
355170 EP. 02/13/1990
465358 EP. 01/13/1992
466569 EP. 01/13/1992

International Class

C07D 333/22

Foreign Application Priority Data

1997-03-05 FR

Abstract

The present invention relates to a process for the preparation of 2-thienylethylamine derivatives of general formula: ##STR1## 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: ##STR2## 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: ##STR3## in which R and R1 have the same meaning as above, in the presence of an alkali metal borchydride of general formula:X--Y IVin which X represents an alkali metal atom and Y represents a group of formula:--BH3 CN or --BH.sub.(4-w) Zwin 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.