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    62.
    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.

    63.
    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.

    66.
    发明专利
    未知

    公开(公告)号：DK131788C

    公开(公告)日：1976-02-09

    申请号：DK569373

    申请日：1973-10-19

    Applicant: HOECHST AG

    Inventor： STACHE U ,  RADSCHEIT K

    IPC: C07J31/00 ,  C07D20060101 ,  C07J1/00 ,  C07J17/00 ,  C07J19/00 ,  C07J21/00

    Abstract: The present invention relates to an improved process for the manufacture of beta -(3-oxo-7 alpha -thioacyl-17 beta -hydroxy-4-androsten-17 alpha -yl)-propionic acid gamma -lactones, in which a beta -(3-oxo-17 beta -hydroxy-4,6-androstadien-17 alpha -yl)-propionaldehyde dialkyl or alkylene acetal is reacted with a thiocarboxylic acid, in a mixture of water an an organic solvent miscible with water, to yield a beta -(3'-oxo-7' alpha -thioacyl-17 beta '-hydroxy-4'-androsten-17 alpha -yl)-propionaldehyde-dialkyl or alkylene acetal and in which this compound is oxidized in an acid solution to yield the corresponding gamma -lactone.

    68.
    发明专利
    未知

    公开(公告)号：FR2100872B1

    公开(公告)日：1975-08-01

    申请号：FR7124832

    申请日：1971-07-07

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J19/00 ,  A61K27/00 ,  C07C169/00 ,  C07C173/00

    Abstract: 1362383 Cardenolides; bufadienolides FARBWERKE HOECHST AG 7 July 1971 [7 July 1970] 31974/71 Heading C2U [Also in Division A5] The invention comprises (A) the compounds 3#,14 - dihydroxy - 5α,14# - bufa - 20,22 - dienolide (Ia); 3#-hydroxy-5α,14α-card-20(22)- enolide; 3# - hydroxy - 5α - bufa - 14,20,22- trienolide; and 3#-hydroxy-5α,14α-bufa-20,22- dienolide; and (B) a process for preparing compounds of formula (wherein R 1 is the lactone ring of a 20(22)- cardenolide or 20,22-bufadienolide; R 2 is CH 3 , CH 2 OH or CH 2 OCOCH 3 ; R 3 is H, OH or acyloxy; R 4 is H; or R 3 + R 4 is epoxy or an extra C-C bond; and R 5 and R 6 are each H, OH or acyloxy) which comprises reducing the corresponding 3-oxo-# 4 compounds (wherein R 2 is alternatively CHO and R 5 and R 6 are each alternatively oxo) with a reducing agent which is more powerful than NaBH 4 , in the presence of an organic nitrogen base at - 30‹ to + 60‹ C. Any oxo groups at positions 11, 12 and 19 are reduced concomitantly. Specified reducing agents are the borohydrides of Li, Mg, Ca, Sr, Ba, Zn and Al, the trimethoxy borohydrides of Na and Li, the aluminium hydrides of Na, Li and Mg, aluminium hydride, lithium trimethoxy aluminium hydride, diborane, pyridine-borane, ethane-1,2- diamine-borane and (3-methyl-2-butyl)borane. Compound Ia supra is alternatively prepared from 3# - hydroxy - 5α - bufa - 14,20,22 - trienolide (III) by the sequence : III # III 3- formate # 15α-bromo-(Ia)-3-formate # Ia 3-formate -# Ia. 3 - Oxo - 14α - bufa - 4,20,22 - trienolide is prepared from the corresponding # 5 -3#-ol by Oppenauer oxidation. Compounds I are said to be cardiotonic, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    CARDENOLIDE DERIVATIVES AND A PROCESS FOR THEIR MANUFACTURE
    69.
    发明专利
    CARDENOLIDE DERIVATIVES AND A PROCESS FOR THEIR MANUFACTURE 未知

    公开(公告)号：GB1363674A

    公开(公告)日：1974-08-14

    申请号：GB4996571

    申请日：1971-10-27

    Applicant: HOECHST AG

    Inventor： STACHE U ,  FRITSCH W ,  HAIDE W ,  RADSCHEIT K ,  LINDNER

    IPC: A61K20060101 ,  A61K31/585 ,  C07C20060101 ,  C07D20060101 ,  C07J17/00 ,  C07J41/00 ,  C07C173/02 ,  A61K27/00

    Abstract: 1363674 3-Aminocardenolides FARBWERKE HOECHST AG 27 Oct 1971 [29 Oct 1970] 49965/71 Heading C2U The invention comprises compounds of formula wherein R 1 is H or C 1-4 aliphatic carboxylic acyl; R 2 and R 3 are each H or OH, or R 2 and R 3 together represent an α- or #-epoxy group or # 14 -unsaturation; R 4 , R 5 and R 7 are each H or free or esterified hydroxyl; R 6 is H or free, esterified or etherified hydroxyl; and R 8 is H or OH; and salts of those compounds wherein R 1 is H. Compounds I are prepared from the corresponding 3-ones (which may also contain a 19- oxo group) by reaction with hydroxylamine or a salt thereof to give a 3-oxime which is reduced using zinc in the presence of an aliphatic carboxylic acid to give a 3-amino and/or 3-acylamino compound I. The 3-acylamino compounds (and mixtures thereof with the 3-amino compounds) may be hydrolysed to give the 3- amino compounds and the latter may be salified or acylated. The inventive compounds are said to be cardiotonic, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    3BETA-HYDROXY-5ALPHA-CARDENOLIDES AND -NUGSFIRNOLIFRD SNF PTOVRDD
    70.
    发明专利
    3BETA-HYDROXY-5ALPHA-CARDENOLIDES AND -NUGSFIRNOLIFRD SNF PTOVRDD 未知

    公开(公告)号：GB1362383A

    公开(公告)日：1974-08-07

    申请号：GB3197471

    申请日：1971-07-07

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J19/00 ,  C07C173/02 ,  A61K27/00 ,  C07C173/04

    Abstract: 1362383 Cardenolides; bufadienolides FARBWERKE HOECHST AG 7 July 1971 [7 July 1970] 31974/71 Heading C2U [Also in Division A5] The invention comprises (A) the compounds 3#,14 - dihydroxy - 5α,14# - bufa - 20,22 - dienolide (Ia); 3#-hydroxy-5α,14α-card-20(22)- enolide; 3# - hydroxy - 5α - bufa - 14,20,22- trienolide; and 3#-hydroxy-5α,14α-bufa-20,22- dienolide; and (B) a process for preparing compounds of formula (wherein R 1 is the lactone ring of a 20(22)- cardenolide or 20,22-bufadienolide; R 2 is CH 3 , CH 2 OH or CH 2 OCOCH 3 ; R 3 is H, OH or acyloxy; R 4 is H; or R 3 + R 4 is epoxy or an extra C-C bond; and R 5 and R 6 are each H, OH or acyloxy) which comprises reducing the corresponding 3-oxo-# 4 compounds (wherein R 2 is alternatively CHO and R 5 and R 6 are each alternatively oxo) with a reducing agent which is more powerful than NaBH 4 , in the presence of an organic nitrogen base at - 30‹ to + 60‹ C. Any oxo groups at positions 11, 12 and 19 are reduced concomitantly. Specified reducing agents are the borohydrides of Li, Mg, Ca, Sr, Ba, Zn and Al, the trimethoxy borohydrides of Na and Li, the aluminium hydrides of Na, Li and Mg, aluminium hydride, lithium trimethoxy aluminium hydride, diborane, pyridine-borane, ethane-1,2- diamine-borane and (3-methyl-2-butyl)borane. Compound Ia supra is alternatively prepared from 3# - hydroxy - 5α - bufa - 14,20,22 - trienolide (III) by the sequence : III # III 3- formate # 15α-bromo-(Ia)-3-formate # Ia 3-formate -# Ia. 3 - Oxo - 14α - bufa - 4,20,22 - trienolide is prepared from the corresponding # 5 -3#-ol by Oppenauer oxidation. Compounds I are said to be cardiotonic, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

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