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 333/32 (2006.01) C07D 409/00 (2006.01) C07F 9/32 (2006.01) C07F 9/40 (2006.01) C07F 9/6553 (2006.01)
Patent
CA 1205809
-37- ABSTRACT The present invention provides a process for the preparation of 2-(thien-2-yl)- and 2-(thien-3-yl)- ethylamine derivatives 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, wherein a compound of the general formula:- Image (II) in which X and Y, which can be the same or different, are alkyl, alkoxy, aryl, aryloxy, diarylamino or dialkylamino radicals, is condensed with a carbonyl compound of the general formula:- Image (III) in which R1 is as defined above, to give a compound of the general formula:- Image (IV) in which X, Y and R1 are as defined above, which is treated with a base B?M? to give a carbanion of the general formula:- Image (V) in which X, Y and R1 are as defined above, which is converted, by the action of heat, into the derivative of the general formula:- Image (VI) in which X, Y and R1 are as defined above, and then, after taking up in water, into a derivative of the general formula:- Image (VII) in which X, Y and R1 are as defined above, which is treated successively with a base B'?M'? and then with a carbonyl compound of the general formula:- Image (VIII) in which Ar and R2 are as defined above, to give a compound of the general formula:- Image (IX) in which R1, R2 and Ar are as defined above, and then, by treatment with a reducing agent, converted into a compound of general formula (I).
406289
Chekroun Isaac
Heymes Alain
Ridout & Maybee Llp
Sanofi
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