C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 75/00 (2006.01) A61P 29/00 (2006.01) C07J 3/00 (2006.01) C07J 5/00 (2006.01) C07J 71/00 (2006.01)
Patent
CA 2450661
Process for preparing flumethasone (6.alpha.,9.alpha.-difluoro- 11(3,17.alpha.,21-trihydroxy-16.alpha.-methyl- pregna-1,4-diene-3,20-dione), flumethasone 21-acetate or its 17-carboxyl androsten analogue of the formula: Image which process comprises (a) reacting a compound of formula (II) Image 18 with benzoyl chloride to form a 3-enolic ester of the formula (IIIa): Image b) reacting the enol benzoate (IIIa) with an electrophilic fluorination agent to introduce fluorine in the C6- position to form a compound of formula (IIIb): Image 19 (c) deprotecting the compound (IIIb) at C3 to form a compound of formula (IV): Image (d) fluorinating the 9,11-epoxy group of compound IV by reacting it with hydrofluoric acid to yield flumethasone 21-acetate; and optionally (e) hydrolysing the flumethasone 21-acetate, in the presence or absence of an oxidising agent, to yield compound (I) or flumethasone, respectively.
L'invention concerne un procédé destiné à préparer du fluméthasone (6a, 9a-difluoro-11 beta , 17a, 21-trihydroxy-16a-méthyl-pregna-1,4-diène-3,20-dione), du fluméthasone 21-acétate ou son analogue 17-carboxyle androstène. Ce procédé consiste à faire réagir un composé de formule (IIIa) avec un agent de fluoration électrophile.
Mendes Zita
Villax Ivan
Hovione Limited
Sim & Mcburney
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