C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 217/20 (2006.01) C07D 213/08 (2006.01)
Patent
CA 2180341
The present invention relates to methods for the production of E-1-[4'-(2-dimethylaminoethoxy)-phenyl]-1-(3'-hydroxyphenyl)-2- phenyl-1-butene of formula (I) which comprises heating the compound of formula (II) (where R is an easily hydrolyzable protecting group) in the presence of an organic solvent and HCl gas and cooling the reaction to obtain the compound of formula (IIIa), and then heating the isolated compound of formula (IIIa) in the presence of sulfuric acid or hydrochloric acid to obtain the compound according to formula (I).
L'invention se rapporte à des procédés de production de E-1-[4'-(2-diméthylaminoéthoxy)-phényl]-1-(3'-hydroxyphényl)-2-phényl-1-butène de la formule (I), consistant à chauffer le composé de formule (II) en présence d'un solvant organique et de gaz HCl, à refroidir la réaction afin d'obtenir le composé de formule (IIIa), puis à chauffer le composé isolé de la formule (IIIa) en présence d'acide sulfurique ou chlorhydrique afin d'obtenir le composé selon la formule (I). Dans la formule (II), R est un groupe protecteur que l'on peut facilement hydrolyser.
Grill Helmut
Woschina Axel
Blake Cassels & Graydon Llp
Klinge Pharma Gmbh
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