C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 301/00 (2006.01) C07B 55/00 (2006.01) C07D 303/08 (2006.01) C07D 405/06 (2006.01) C07D 417/06 (2006.01)
Patent
CA 2629092
Disclosed is a process for the manufacture of a Compound of formula (I) wherein Hal represents fluoro or chloro, and R1 and R2 represent, independently from one another, hydrogen or HaI; in which process a Compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ester in a polar non-nucleophilic solvent at a temperature of -10 to 50~C to give the Compound of formula (I).
L'invention concerne un procédé destiné de production d'un composé de la formule (I) où Hal représente fluoro ou chloro, et R1 et R2 réprésentent, indépendamment l'un de l'autre, un hydrogène ou HaI. Dans ce procédé, un composé de la formule (II) est converti en ester d'acide sulfonique alkyle, fluoroalkyle ou aryle correspondant, que l'on fait ensuite réagir avec un nitrure de métal alcalin en présence d'un ester couronne ad hoc dans un solvant non nucléophile polaire à une température de -10 à 50 °C pour obtenir le composé de la formule (I).
Muller Marc
Xu Lin
Basilea Pharmaceutica Ag
Gowling Lafleur Henderson Llp
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