专利摘要:
New spirolactones of the formula <IMAGE> (I) wherein <IMAGE> +tr <IMAGE> R is a lower alkyl of up to 5 carbon atoms, and <IMAGE> +tr <IMAGE>
公开号:SU743582A3
申请号:SU792706061
申请日:1979-01-11
公开日:1980-06-25
发明作者:Вихерт Рудольф;Биттлер Дитер;Керб Ульрих;Казальс-Штенцель Ерге;Лозерт Вольфганг
申请人:Шеринг Аг (Фирма);
IPC主号:
专利说明:

one
This invention relates to a process for the preparation of novel spirolactones of general formula I:
GT
.
COR
R is alkyl,
where / choose from groups, formulas
- /. v ™ v
having pharmacological activity ll.
The use of the known method of thioacylation of olefins with thioalkanoic acids fij makes it possible to produce new steroid spirolactones of the general formula (I)
The purpose of the invention is to obtain new steroid spirolactones exhibiting pharmacological activity. This is achieved by the fact that Lb-unsaturated spirolactones of the general formula I I
-P
ten
where C has the indicated meanings
treated with thioalkanoic acid
15 HSCOR, where R has the above meaning in a proton solvent, usually methanol, at the boiling point of the reaction mass, followed by separating the desired product
known methods.
Example 1. 1.5 g of 3-oxo-4, 6,15-androstrieno- (17) 0-1 (spiro-5) -perhydrofuran-2-one in 22.5 ml of methanol is boiled under reflux for 35 2 hours along with 1.5 MP of thioacetic acid. It is then diluted with ether, water, sodium bicarbonate solution and water, dried and evaporated. The residue hrsmatog30 is refined on silica gel.
权利要求:
Claims (1)
[1]
Claim
1. The method of producing spirolactones of General formula I:
where, R ^ - ar ^ kil C / -Cg is selected from the group of formulas
N — I iki) ~ 1
CH 2 GH 2.
wherein the Δ6 - unsaturated spirolactone ob- where "J has the abovementioned meaning, PY 16 C was treated tioalkanovoy acid of formula 45 HSCOR, where R has the abovementioned meaning, in a protic solvent at the reflux temperature of the reaction mass and recovering the desired product.
类似技术:
公开号 | 公开日 | 专利标题
SU743582A3|1980-06-25|Spirolactone producing method
Doerschuk1952|Acyl migrations in partially acylated, polyhydroxylic systems1
Marshall et al.1971|Total synthesis of |-isonootkatone. Stereochemical studies of the Robinson annelation reaction with 3-penten-2-one
Wendler et al.1952|The Synthesis of 11-Hydroxylated Cortical Steroids. 17-Hydroxycorticosterone1
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同族专利:
公开号 | 公开日
IT1092262B|1985-07-06|
DE2652761A1|1978-05-18|
GB1550568A|1979-08-15|
ES464193A1|1978-09-01|
IL53353A|1982-04-30|
GR65227B|1980-07-30|
AU512611B2|1980-10-16|
HU174983B|1980-04-28|
SU695560A3|1979-10-30|
CA1092094A|1980-12-23|
JPH0242840B2|1990-09-26|
DE2652761C2|1985-11-21|
JPS5363373A|1978-06-06|
SE7712891L|1978-05-17|
SE436425B|1984-12-10|
DD132968B3|1991-03-28|
AT356827B|1980-05-27|
IE46076B1|1983-02-09|
CH631463A5|1982-08-13|
ATA815577A|1979-10-15|
CS194823B2|1979-12-31|
IL53353D0|1978-01-31|
JPS61218595A|1986-09-29|
BE860877A|1978-05-16|
LU78514A1|1978-03-20|
FR2370755A1|1978-06-09|
NL7711946A|1978-05-18|
DD132968A5|1978-11-22|
FR2370755B1|1980-06-06|
DK141967B|1980-07-28|
IE46076L|1978-05-16|
DK141967C|1980-12-08|
AU3050977A|1979-05-17|
US4129564A|1978-12-12|
CH632774A5|1982-10-29|
JPS6156240B2|1986-12-01|
DK508077A|1978-05-17|
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法律状态:
优先权:
申请号 | 申请日 | 专利标题
DE2652761A|DE2652761C2|1976-11-16|1976-11-16|15,16-methylene-spirolactones, processes for their preparation and pharmaceuticals containing them|
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