C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 31/00 (2006.01) A61K 31/56 (2006.01) A61P 5/44 (2006.01)
Patent
CA 2654644
The present invention relates to a process for the preparation of steroidal 17.beta.-carboxylic thioates. More particularly the present invention relates to a convenient and efficient synthesis of steroidal 17.beta.-carboxylic thioates, such as fluticasone propionate formula (I), using soluble mixed fluorides to introduce fluorine by displacing an appropriate leaving group X in compounds formula (II) resulting in selective and controlled fluorination. The present invention also relates to intermediates formula (II) and their preparation.
La présente invention concerne un procédé de préparation de thioates 17.beta.-carboxyliques stéroïdiens. L'invention concerne plus particulièrement une synthèse pratique et efficace de thioates 17.beta.-carboxyliques stéroïdiens, par exemple le propionate de fluticasone de formule (I), à partir d'un mélange de fluorures solubles afin d'introduire du fluor en déplaçant un groupe labile X approprié dans des composés de formule (II), selon un procédé de fluoration sélectif et contrôlé. La présente invention concerne également des intermédiaires de formule (II) et leur préparation.
Gadakar Mahesh
Gore Vinayak G.
Pokharkar K.
Wakchure V.
Gadakar Mahesh
Generics [uk] Limited
Gore Vinayak G.
Merck Development Centre Private Limited
Osler Hoskin & Harcourt Llp
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