METHOD OF THIOCARBOXYLIC ACID ETHERIFICATION Russian patent published in 2009 - IPC C07J31/00 

Abstract RU 2351605 C2

FIELD: chemistry.

SUBSTANCE: there is disclosed improved method of producing connection of formula [II] , being intermediate in fluticasone propionate synthesis by etherification of C-17 hydroxyl group 6α,9α-difluoro-11β, 17α-dihydroxy-16α-methyl-3-oxoandrosta-1,4-diene-17β-thiocarboxylic acid, compound of formula [I] . Method involves processing of compound [I] with small excess of carboxylic acid chloranhydride of general formula R-COCl where R stands for -CH2CH3, -CH2CH2CH3 or -CH(CH3)2, in inert solvent, with tertiary amine added. Preferentially, method is enabled with using pyridine with acetone added at temperature 5°C to -20°C.

EFFECT: method enables to eliminate intermediate byproduct.

13 cl, 3 ex

Similar patents RU2351605C2

Title Year Author Number
METHOD FOR OBTAINING FLUTICASONE PROPIONATE OBTAINING, PARTICULARLY POLYMORPHOUS FORM 1 2003
  • Kut Stiven Dzhon
  • Najs Rozalin Kehj
  • Vipperman Mark Dejvid
RU2333218C2
SPECIFIC GLYCOCOTRICOSTEROID COMPOUND WITH ANTIINFLAMMATORY EFFECT 2004
  • Biggadajk Kejt
  • Dzhon Meht'Ju Piter
  • Nidkham Debora
RU2348645C2
METHOD FOR OBTAINING 6α, 9α-DIFLUOR- 17α-(1-OXO-PROPOXY)-11β-HYDROXY-16α-METHYL-3-OXO-ANDROST-1,4-DIENE-17β-CARBOTHIONE ACID 2003
  • Kut Stiven Dzhon
  • Najs Rozalin Kehj
  • Uipperman Mark Dejvid
RU2333217C2
DERIVATIVES OF ANDROSTENE, PHARMACEUTICAL COMPOSITION 1997
  • Bodor Nikolas S.
RU2194053C2
CHEMICAL COMPOUNDS 2008
  • Miren Finn
  • Sandvol'D Marit Liland
  • Ehriksen Ole Khenrik
  • Khagen Stejnar
RU2462472C2
SPECIFIC GLYCOCORTICOSTEROID COMPOUND WITH ANTIINFLAMMATORY EFFECT 2004
  • Biggadajk Kejt
  • Nidkham Debora
RU2359973C2
16α,17a-ACETAL-SUBSTITUTED ANDROSTANE-17b-CARBOXYLIC ACID ESTERS OR THEIR STEREOISOMERS 1991
  • Pol Khehkan Andersson[Se]
  • Per Tur Andersson[Se]
  • Bror Arne Talen[Se]
  • Jan Vill'Jam Trofast[Se]
  • Bengt Ingemar Aksel'Sson[Se]
RU2081879C1
METHOD FOR PREPARING FLUMETASONE, COMPOUND 2002
  • Vilaks Ivan
  • Mendish Zita
RU2260596C1
APPLICATION OF H, K-ATPase INHIBITOR FOR TREATING NASAL POLYPS 1997
  • Lindberg Per
  • Pinas-Masso Khoan
  • Serra-Karreras Khordi
  • Trofast Jan
RU2197966C2
STEROID ESTERS OR THEIR STEREOISOMERS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION 1992
  • Bengt Aksel'Sson
  • Ral'F Brattsand
  • Lejf Kell'Strem
  • Arne Talen
RU2112775C1

RU 2 351 605 C2

Authors

Sobral Luish

Martin Dionisio

Kheggi Uil'Jam

Lejtan Ehmilija

Dates

2009-04-10Published

2004-12-02Filed