Process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl
AssigneeSanofi
InventorsJanos Fazekas, Peter Miskolczi, Annamaria Molnar, Bela Agai, Zsolt Parkanyi
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Abstract
The present invention is a process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine as set forth in formula (I) and new intermediates of the preparation process.
Claims13
A process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine of formula (I)
- the process comprising
- a.) reacting a compound of formula (II)
- wherein X represents a halogen, with an alkali metal-thiocyanate, in the presence of a phase transfer catalyst, to obtain a 2-thiocyanato-1-(2-chloro-4-methoxy -5-methylphenyl)-propan-1-one of formula (III)
- or a tautomeric form thereof;
- and
- b) reacting said compound of formula (III) or tautomeric form thereof with 2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl-amine of formula (IV)
- to form the compound of formula (I).
A 2-thiocyanato-1-(2-chloro-4-methoxy-5-methylphenyl) -propan-1-one of formula (III)
- or a tautomer thereof.
A process for the preparation of 2-thiocyanato-1-(2-chloro-4-methoxy-5-methylphenyl)-propan-1-one of formula (III)
- the process comprising reacting a compound of formula (II)
- where X represents a halogen, with an alkali metal-thiocyanate, in the presence of a phase transfer catalyst.
A process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazol-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methyl -phenyl)-ethyl]-amine of formula (I)
- the process comprising reacting 2-thiocyanato-1-(2-chloro-4-methoxy -5-methyl-phenyl)-propan-1-one of formula (III)
- with 2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl-amine of formula (IV)
- wherein the compound of formula (III) is added to the compound of formula (IV).
Dependencies are inferred from the claim text.