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    61.
    发明专利
    未知

    公开(公告)号：SE353534B

    公开(公告)日：1973-02-05

    申请号：SE534069

    申请日：1969-04-16

    Applicant: HOECHST AG

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

    IPC: A61K31/573 ,  A61K31/58 ,  C07C169/00

    Abstract: DELTA 14-20-KETO-21-DIALKOXY STEROIDS ARE PREPARED BY OXIDIZING 20-KETO-15 alpha ,21-DIHYDROXY STEROIDS OF THE GENERAL FORMULA IN WHICH Y is an oxo group which may be ketalized, GROUP WHICH MAY BE ETHERIFIED OR ESTERIFIED, A DELTA 3-, DELTA 2-, OR DELTA 3,5-ENOL ETHER GROUP OR A DELTA 3-, DELTA 2-, OR DELTA 3,5-ENAMINO GROUP, WHICH GROUPS MAY HAVE A DOUBLE BOND IN THE 4-POSITION, AND IS A LOWER ACYCLIC OR CYCLIC ACETAL GROUPING, ACETALIZING THE 15 alpha -HYDROXY-20-KETO-21-OXO STEROIDS OBTAINED, REACTING THE 15 alpha -HYDROXY-20-KETO-21-DIALKOXY STEROIDS THUS OBTAINED WITH SULFONIC ACID HALIDES AND TREATING THE 15-SULFONIC ACID ESTERS THUS OBTAINED WITH AGENTS SPLITTING OFF ACIDS. The products are valuable intermediates for the manufacture of medicaments.

    64.
    发明专利
    未知

    公开(公告)号：DK123477B

    公开(公告)日：1972-06-26

    申请号：DK98871

    申请日：1971-03-03

    Applicant: HOECHST AG

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

    IPC: C07J19/00 ,  C07J75/00 ,  C07C173/02

    Abstract: 1,184,238. 15α - Halo - 14# - hydroxy - cardenolides. FARBWERKE HOECHST A.G. 30 Nov., 1967 [30 Nov., 1966], No. 54506/67. Heading C2U. Novel 3# - formoxy - 15α - halo - 14# - hydroxy - 5# - card - 20(22) - enolides are prepared by reducing with a complex metal halide a 3- keto - 5# - carda - 14,20(22) - dienolide to obtain the corresponding 3α-hydroxy compound which is converted to a 3-sulphonic ester. This ester is treated with alkali metal formate, formic acid, water, and dimethylformamide to obtain a 3#-formoxy - 5# - carda - 14,20(22) - dienolide, and the addition of hypohalous acid across the 14,15-double bond of latter yields the desired product. The starting-material may contain further substituents, e.g. alkyl or acyloxy groups at positions 1, 2, 4, 7, 11, 12, 16 or 17.

    67.
    发明专利
    未知

    公开(公告)号：DE2033599A1

    公开(公告)日：1972-01-20

    申请号：DE2033599

    申请日：1970-07-07

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J19/00 ,  C07C173/02

    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.

    68.
    发明专利
    未知

    公开(公告)号：BE769567A

    公开(公告)日：1972-01-06

    申请号：BE769567

    申请日：1971-07-06

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J19/00 ,  C07D

    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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