11,21-DIACETATE (22RS)-16α,17α-BUTYLIDENEDIOXY-1111β, 21-DIHYDROXYPREGNA-1,4-DIENE-3,20-DIONE AS INTERMEDIATE PRODUCT IN SYNTHESIS OF BUDECONIDE Russian patent published in 1994 - IPC

Abstract SU 1660379 A1

FIELD: steroid compounds, more particularly (22RS-16α; 17α-butylidenedioxy-11β, 21-dihydroxypregna-1,4-diene-3.20-dione 11,21-diacetate as an intermediate product in the synthesis of budeconide. SUBSTANCE: the semifinished product is synthesized by acetalization of 16α-oxyprednisolone 11.21-diacetate with butyric aldehyde in a CH2Cl2 solution in the presence of a HClO4 catalyst. The yield 96.5%, mp 118-128 C after decrystallization 150-160 C; [α]2D

0= + 108°, the empirical formula 1: C29H38O8. The new semifinished product makes it possible to obtain industrial budeconide by a microbiological method (using the culture coryn mediolanum( with a yield of 100%; after the purification the yield 70%, and the total yield as calculated for prednisolone about 43%; this is by 2 times higher than in the prior art. EFFECT: a new semifinished product for the synthesis of effective broncholitic with high yield.

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SU 1 660 379 A1

Authors

Gireva N.N.

Demchenko В.I.

Кrymov А.Р.

Navtsenja L.G.

Naumova G.А.

Мart'Janova V.V.

Domrachev N.V.

Shashkina L.F.

Sherman F.В.

Кarina L.М.

Dates

1994-09-30Published

1989-07-27Filed