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    Process for the manufacture of pregnane-20-one-3beta,5beta,14beta,21-tetrol
    12.
    发明授权
    Process for the manufacture of pregnane-20-one-3beta,5beta,14beta,21-tetrol 失效
    制备PREGANAN-20-ONE-3BETA，5BETA，14BETA，21-TETROL的方法

    公开(公告)号：US3732210A

    公开(公告)日：1973-05-08

    申请号：US3732210D

    申请日：1971-01-26

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J5/00 ,  C07J71/00 ,  C07C173/00

    CPC classification number: C07J17/00

    Abstract: A PROCESS FOR THE MANUFACTURE OF PREGNANE-20-ONE3B,5B,14B,21-TETROL, USEFUL AS A STARTING MATERIAL FOR PHARMACEUTICALLY VALUABLE COMPOUNDS OF THE PREGNANE SERIES, BY CONVERTING $414-PREGNADIENE-3,20-DIONE-21-OL TO THE CORRESPONDING 3,20-BIS-ALKYLENE-DIOXY-$5,14-PREGNADIENE21-OL WIT ETHYLENE GLYCOL OR NEOPENTYL GLYCOL, ACYLATING TO FORM THE 21-ACYLATE AND THEN PARTIALLY DE-KETALIZING THE ACYLATE TO PRODUCE 20-ALKYLENE-DIOXY-$4,14-PREGNADIENE-3ONE-21-ACYLATE, REDUCING THE 3-KETO GROUP WITH AN ORGANOMETALLIC REDUCING AGENT, WHEREBY THE 21-ACYLATE GROUP MAY ALSO BE CONVERTED BY THE REDUCING AGENT TO THE 21-OL, ACYLATING THE 20-ALKYLENE-DIOXY-$4,14-PREGNADIENE-3,21-DIOL OR -3-OL-21-ACYLATE TO FORM 20-ALKYLENE-DIOXY-$4,14PREGNADIENE-3,21-DIACYLTE, TREATING THIS WITH HYPOBROMOUS ACID TO FORM 5A,15A-DIBROMO-20-ALKYLENE-DIOXY-PREGNANE-3B,5B,14B,21-TETROL-3,21-DIACYLATE AND DEBROMINATING WITH A BASE TO FORM 20-ALKYLENE-DIOXY-4B(5B), 14B(15BDIOXIDO-PREGNANE-3B,21-DIOL OR THE CORRESPONDING -3,21-DIACYLATE, AND REDUCING TO 20-ALKYLENE-DIOXY-PREGNANE-3B, 5B,14B,21-TETROL WITH AN ORGANOMETALLIC REDUCING AGENT. THE 20-ALKYLENE-DIOXY GROUP IS HYDROLYZED TO FORM THE DESIRED PREGNANE 20-ONE-3B,5B,14B,21-TETROL, WHICH MAY BE FURTHER REATED WITH DIHYDROPYRANE TO FORM THE CORRESPONDING -3B,21-DITETRAHYDROPYRANYL ETHER.

    3-n-alkyl-amino-cardenolides and process for their manufacture
    13.
    发明授权
    3-n-alkyl-amino-cardenolides and process for their manufacture 失效
    3-N-烷基 - 氨基甲酸酯及其制备方法

    公开(公告)号：US3725393A

    公开(公告)日：1973-04-03

    申请号：US3725393D

    申请日：1971-10-18

    Applicant: HOECHST AG

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

    IPC: A61K20060101 ,  C07D20060101 ,  C07J19/00 ,  C07C173/02

    CPC classification number: C07J75/00

    Abstract: 3-N-alkyl-amino-cardenolides of the general formula

    Abstract translation: 其中R 1表示氢或β-羟基的通式的3-N-烷基 - 氨基 - 己烯酸烯; R 2和R 3各自表示氢或羟基，或者R 2和R 3一起代表另外的C-C键或α或β-氧代基; R4，R5，R6和R7各自表示氢或可被酯化的羟基 - R6的OH-基团也可以醚化 - ; R8代表氢或羟基; 并且R 9表示可以含有一个或多个OH-基团的碳原子数1〜6的烷基或芳脂肪族基团，及其与无机酸或有机酸的盐。 这些化合物具有有价值的药理学性质，特别是正或负性肌力作用，并且在脂质中具有显着改善的溶解性。

    18.
    发明专利
    未知

    公开(公告)号：ATA583871A

    公开(公告)日：1976-06-15

    申请号：AT583871

    申请日：1971-07-06

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J19/00

    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.

    20.
    发明专利
    未知

    公开(公告)号：CH562259A5

    公开(公告)日：1975-05-30

    申请号：CH983871

    申请日：1971-07-05

    Applicant: HOECHST AG

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

    IPC: C07D20060101 ,  C07J19/00

    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.

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