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    34.
    发明专利
    未知

    公开(公告)号：SE352349B

    公开(公告)日：1972-12-27

    申请号：SE1282569

    申请日：1969-09-18

    Applicant: HOECHST AG

    Inventor： HAEDE W ,  STACHE U ,  RADSCHEIT K ,  FRITSCH W ,  SCHROEDER H

    IPC: C07C169/28

    Abstract: 1288414 Steroid 21-cyclobutane esters FARBWERKE HOECHST AG 22 Sept 1969 [20 Sept 1968] 46559/69 Heading C2U The invention comprises compounds of formula represents (i) a Y . . . C 9 -C 11 =X group where Y is H or F and X is H 2 , OXO, H(#-OH), H(α-OH), H(#-Cl) or H(#-F), or group; R 1 represents H 2 , H(α-Me), H(#-Me), H(α-F), H(#-F), CH 2 , CHF or CF 2 ; R 2 represents H or OH; R 3 represents a direct bond or a C 1-5 divalent aliphatic hydrocarbon group; and R 4 represents a cyclobutyl group which is substituted by at least one fluorine atom and which may be further substituted by one or more methyl groups and/or chlorine atoms. Preparation of the above compounds is from the corresponding steroid 21-ols by reaction with a compound of formula Cl-CO-R 3 -R 4 . Product interconversions specified are 1,2- and/ or 6,7-dehydrogenation; 6-, 9-, 11- and/or 16- fluorination; further fluorination of the cyclobutane ring; and reduction of 11-oxo to 11- hydroxy. The inventive compounds are stated to possess anti-inflammatory activity and may be made up with carriers into pharmaceutical and veterinary compositions for topical administration.

    36.
    发明专利
    未知

    公开(公告)号：FI45756B

    公开(公告)日：1972-05-31

    申请号：FI86169

    申请日：1969-03-24

    Applicant: HOECHST AG

    Inventor： HAEDE W ,  RADSCHEIT K ,  STACHE U ,  FRITSCH W

    IPC: A61K31/70 ,  C07C173/02

    Abstract: 1,228,069. Cardenolide ethers. FARBWERKE HOECHST A.G. 2 April, 1969 [6 April, 1968], No. 17192/69. Heading C2U. The invention comprises compounds of formula wherein R 1 is x-H, #-H or #-OH; R 2 , R 3 and R 4 are each H or OH; and R 5 is C 1-3 alkyl; and their preparation by LiAlH 4 reduction of compounds of formula wherein R 6 is C 1-3 alkyl and R 7 is CH 3 , CH 2 OH or CHO. A starting material with R 7 = CHO yields a product with R 2 = OH. Compounds of Formula II are prepared from the corresponding 3-hydroxy steroids by reaction with appropriately substituted dihydropyrans. Compounds of Formula I are stated to possess inotropic, cardiovascular, diuretic and anti-diarrhoeal effects, and may be made up with carriers into pharmaceutical compositions for oral administration.

    2,3-ALKYLIDENE-RHAMNOPYRANOSIDES AND PROCESS FOR PREPARING THEM
    37.
    发明专利
    2,3-ALKYLIDENE-RHAMNOPYRANOSIDES AND PROCESS FOR PREPARING THEM 未知

    公开(公告)号：ZA712827B

    公开(公告)日：1972-01-26

    申请号：ZA712827

    申请日：1971-04-30

    Applicant: HOECHST AG

    Inventor： HAEDE W ,  STACHE U ,  LINDNER E ,  FRITSCH W ,  RADSCHEIT K

    IPC: C07J19/00 ,  C07G ,  A61K

    Abstract: 1345388 Convallatoxin derivatives FARBWERKE HOECHST AG 30 April 1971 [2 May 1970] 12427/71 Heading C2U The invention comprises compounds of formula (wherein R 1 and R 2 are each C 1-4 alkyl, or together with the intervening carbon atom form a carbocyclic or heterocyclic ring; and R 3 is CHO or CH 2 OH) and their preparation from convallatoxin by reaction with R 1 R 2 C(OR 4 ) 2 (where R 4 is C 1-4 alkyl), optionally followed by reduction of 19-oxo to hydroxy. The inventive compounds are said to be cardioactive, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    39.
    发明专利
    未知

    公开(公告)号：SE331279B

    公开(公告)日：1970-12-21

    申请号：SE1718666

    申请日：1966-12-15

    Applicant: HOECHST AG

    Inventor： FRITSCH W ,  HAEDE W ,  RUSCHIG H ,  RADSCHEIT K ,  STACHE U

    IPC: C07J5/00 ,  C07J75/00 ,  C07C167/14

    Abstract: 1,172,237. # 14 -21 -Acyloxy-pregnenes. FARBWERKE HOECHST A.G. 19 Dec., 1966 [18 Dec., 1965], No. 56726/66. Heading C2U. A # 14 - 3,20 - diketo - 21 - acyloxy - 5#- pregnene or a # 4,14 -3,20-diketo-21-acyloxypregnadiene is obtained by reacting a 3,20- diketo - 15α,21 - dihydroxy - 5# - pregnane or a # 4 - 3,20 - diketo - 15α,21 - dihydroxy - pregnene with a sulphonic acid halide, treating the 15α,21 - disulphonate or 15α - disulphonate- 21-halide so obtained with an alkali metal salt of a carboxylic acid in the presence of an organic solvent, and treating the resulting 21- acyloxy-15α-sulphonate with an agent capable of splitting off sulphonic acids.

    40.
    发明专利
    未知

    公开(公告)号：SE314367B

    公开(公告)日：1969-09-08

    申请号：SE324267

    申请日：1967-03-09

    Applicant: HOECHST AG

    Inventor： FRITSCH W ,  STACHE U ,  HAEDE W ,  RADSCHEIT K

    IPC: C07J19/00 ,  C07J75/00 ,  C07C167/20

    Abstract: Method for (I) The nucleus may be further substituted and/or unsatd. Intermediate for cardenolides. Crude DELTA4-pregnene-15alpha, 21-diol-3,20-dione-15,21-dimethanesulphonate (from 4.25 g of the 15alpha, 21-diol, 7.3 ml MeSO2Cl, and 14.5 ml C5H5N), D.M.F (40 ml.), and potassium ethyl malonate (5.6 g), were stirred 3 hr. at 60 deg. under N2, cooled, poured into H2O (200 ml), extd. with CH2Cl2/Et2O, washed 6 x with H2O, dried, and evapd. in vac. The residue was dissolved in collidine (41 ml) with warming, cooled to 20 deg., and left for 1 hr. H2O (8 drops) and p-toluene-sulphonic acid (12 g) were added, heated 3-5 min. at 100 deg., refluxed (bath temp. 205 deg.) 50 min., and evapd. in vac. The residue was extd. with d. HCl and CH2Cl2, the organic phase washed (d. HCl and H2O), dried, evapd. in vac., and recryst. from CH2Cl2/MeOH, giving (I) (2.38 g) m.p 275-8 deg.

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