C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/328.2, 260/2
C07D 333/04 (2006.01) C07D 333/20 (2006.01) C07D 409/00 (2006.01) C07F 9/40 (2006.01) C07F 9/6553 (2006.01)
Patent
CA 1205808
The present invention provides a process for the preparation of 2-(thienyl-2)- and 2-(thienyl-3)-ethyl- amines of the general formula:- Image (I) in which R1, which is in the 2-, 3-, 4- or 5-position, is a hydrogen atom, a straight-chained or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or polysubstituted, or R1 is an alkoxy radical, a halogen atom or a nitro, carboxyl, cyano or amino group; the aminoethyl chain is in the 2- or 3-position of the thiophene nucleus; R2 is a hydrogen atom or a straight-chained or branched alkyl radical or a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly- substituted; and Ar is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly- substituted, wherein a carbanion of the general formula:- Image (V) in which X and Y, which may be the same or different, are alkyl, aryl, alkoxy, aryloxy, dialkylamino or diarylamino radicals and R1 has the same meaning as above, is converted by the action of heat into a compound of the general formula:- Image (VI) in which R1, X and Y have the same meanings as above, which, after taking up in water, gives a compound of the general formula:- Image (VII) in which R1, X and Y have the same meanings as above, reduction of which gives a compound of the general formula:- Image (VIII) in which R1, X and Y have the same meanings as above, which is first reacted with a base of the general formula B'?M'? and then with a halogen derivative of the general formula:- Ar-CHX-R2 (IX) in which Ar and R2 have the same meanings as above and X is a halogen atom, to give a compound of the general formula:- Image (x) in which Ar, R1, R2, X and Y have the same meanings as above, which is finally converted into a compound of general formula (I) by the action of an acid.
406266
Chekroun Isaac
Heymes Alain
Ridout & Maybee Llp
Sanofi
LandOfFree
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