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    12.
    发明专利
    未知

    公开(公告)号：SE402294B

    公开(公告)日：1978-06-26

    申请号：SE7408893

    申请日：1974-07-05

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURST A ,  LABLER L ,  MEIER W ,  MULLER P ,  SCOTT J W ,  WIDMER E

    IPC: A61K31/5685 ,  C07J1/00 ,  C07J15/00

    Abstract: 1336894 De-A-9#-steroids F HOFFMANNLA ROCHE & CO AG 21 May 1971 [21 May 1970] 16377/71 Heading C2C The invention comprises certain de-A-9#- steroids of Formula I below, and a process for preparing de-A-9#-steroids in general (which may be optically active or racemic) by hydrogenating the corresponding de-A-# 9 -steroids in an organic solvent with a palladium catalyst in the presence of hydrogen bromide. In some cases acyloxy groups in the starting materials may be converted simultaneously to hydroxyl groups. Hydroxyl groups in the products may subsequently be esterified. The products may be purified from the 9α-isomers which may be formed in minor amounts in the hydrogenation by fractional crystallization or by refluxing in hexane (Example 6). Preferred products have the formula wherein R 1 is C 1-8 alkyl; R 2 is H, C 1-8 alkyl, 3- oxobutyl, ketalized 3-oxobutyl, 3-chlorobut-2- enyl, 2-carboxyethyl, 2-alkoxycarbonyl-ethyl, 2-cyanoethyl, or a group of formula wherein R 3 and R 4 are identical C 1-8 alkyl groups, or one is H and the other is C 1-8 alkyl; and D is a grouping of formula wherein Z is a carbonyl group or a grouping of formula wherein R 5 is free/etherified/esterified hydroxyl; R 6 is H or C 1-8 alkyl; R 7 is H or OH; R 8 is H, OH or C 1-8 alkyl; and R 9 is free/esterified hydroxyl. Compounds of Formula I claimed per se are those wherein R 2 is 3-oxobutyl, ketalized 3- oxobutyl, 3 - chlorobut - 2 - enyl, 2 - carboxyethyl and 2-alkoxycarbonyl-ethyl. Compounds of Formula I may be converted into tetracyclic 9#,10α-steroids as described in Specification 1,336,895 and in Belgian Specifications 697,157 and 742,090 (U.K. equivalents 1,155,511 and 1,298,214). Trans - anti - 6 - (2 - carboxyethyl) - 3amethyl - 3,7 - dioxo - 1,2,3a,4,5,7,8,9,9a, 9bdecahydro - 3H - benz[e]indene (XI) is prepared from 5,5-ethylenedioxy-nonanedinitrile (X) by the sequence: X -# 5-oxo-nonanedinitrile -# 5 - hydroxy - nonanedinitrile -# 8- cyano - 5 - octanolide -# 6 - (3 - cyanopropyl)- 2 - (2 - diethylaminoethyl) - tetrahydropyran - 2- ol -# 3 - (3 - cyanopropyl) - 6a - methyll,2,3,5,6,6a - hexahydro - cyclopenta[f][l]- benzopyran - 7(8H) - one -# 3 - (3 - cyanopropyl)- 6a - methyl - 1,2,3,5,6,6a,7,8 - octahydro - cyclopenta[f][l]benzopyran - 7# - ol -# 6a,9a - trans- 3 - (3 - cyanopropyl) - 6a - methyl - 1,2,3,5,6,6a- 7,8,9,9a - decahydro - cyclopenta[f][l]benzopyran - 7# - ol -# 4 - (6 - cyano - 3 - oxo - hexyl)- 7α - methyl - perhydroindane - 1,5 - dione -# trans - anti - 6 - (2 - cyanoethyl) - 3a - methyl- 3,7 - dioxo - 1,2,3a,4,5,7,8,9,9a,9b - decahydro- 3H-benz[e]indene -# XI.

    15.
    发明专利
    未知

    公开(公告)号：SE7701957L

    公开(公告)日：1977-08-24

    申请号：SE7701957

    申请日：1977-02-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURST A ,  GUTZWILLER J ,  MULLER M ,  WIECHERT R ,  EDER U ,  NEEF G

    IPC: C07J63/00

    Abstract: D-homosteroids of the formula WHEREIN R3 alpha is hydrogen, R3 beta is hydroxy, lower alkanoyloxy or aroyloxy and R3 alpha and R3 beta taken together are oxo; R17a alpha is hydrogen, lower alkyl, ethynyl, vinyl, allyl, methallyl, propadienyl, 1-propynyl, butadiynyl or chloroethynyl; R17a beta is hydrogen, alkanoyl, aroyl, lower alkyl, cycloalkyl-lower-alkyl, benzyl, furfuryl or tetrahydropyranyl; R18 is hydrogen or methyl and the dotted line in the C-ring denotes an additional carbon to carbon bond in the 11,12-position and PROCESSES FOR THE PREPARATION THEREOF ARE DISCLOSED.

    D-HOMO STEROIDS AND PHARMACEUTICAL PREPARATION THEREOF
    16.
    发明专利
    D-HOMO STEROIDS AND PHARMACEUTICAL PREPARATION THEREOF 未知

    公开(公告)号：PH10616A

    公开(公告)日：1977-07-19

    申请号：PH16316

    申请日：1974-09-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： ALIG L ,  WIECHERT R ,  MULLER M ,  KERB U ,  FURST A ,  KELLER P

    IPC: A61K31/56 ,  A61K31/585 ,  C07J63/00 ,  C07J1/00

    Abstract: 1450884 D-homosteroids F HOFFMANNLA ROCHE & CO AG 25 Sept 1974 [26 Sept 1973] 41706/74 Heading C2U The invention comprises compounds of formula wherein the 1,2-bond is single, R 10 being H or Me, or double, R 10 being Me; the 6,7-bond is single, R 7 being H, mercapto, acylthio, alkylthio, cycloalkylthio or aralkylthio, or double, R 7 being H; and the 16,17-bond is single or double. Compounds I (R 7 =H) are prepared (a) from the corresponding # 5 (or # 5,16 )-3#-ols by oxidation to give a # 4 , # 4,6 or # 1,4,6 -3-oxo grouping, e.g. with CrO 3 , DCC/DMS, SO 3 /py, Br 2 /LiBr/Li 2 CO 3 /DMF or with Al(OPr i ) 3 or Al(OBu t ) 3 optionally in the presence of DDQ; or (b) from the corresponding # 5(10) or # 5(10) , 16 -3- ones by acid or base # 5(10) ## 4 isomerization; and are interconvertible by chemical or microbial 1,2- and/or 6,7-dehydrogenation. Compounds I (R 7 is other than H) are prepared from the corresponding 6,7-dehydro compounds (where R 7 =H) by reacting with H 2 S, a mercaptan or a thiocarboxylic acid, optionally followed by 1,2-dehydrogenation. The starting materials are prepared as described in Specifications 1,450,885 and 1,450,886. Compounds I are said to affect body mineral reserves, and may be made up with carriers into pharmaceutical compositions for oral, parenteral rectal and topical administration.

    20.
    发明专利
    未知

    公开(公告)号：SE7411948L

    公开(公告)日：1975-03-27

    申请号：SE7411948

    申请日：1974-09-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： ALIG L ,  FURST A ,  KELLER P ,  MULLER M ,  KERB U ,  WIECHERT R

    IPC: A61K31/56 ,  A61K31/585 ,  C07J63/00

    Abstract: 1450884 D-homosteroids F HOFFMANNLA ROCHE & CO AG 25 Sept 1974 [26 Sept 1973] 41706/74 Heading C2U The invention comprises compounds of formula wherein the 1,2-bond is single, R 10 being H or Me, or double, R 10 being Me; the 6,7-bond is single, R 7 being H, mercapto, acylthio, alkylthio, cycloalkylthio or aralkylthio, or double, R 7 being H; and the 16,17-bond is single or double. Compounds I (R 7 =H) are prepared (a) from the corresponding # 5 (or # 5,16 )-3#-ols by oxidation to give a # 4 , # 4,6 or # 1,4,6 -3-oxo grouping, e.g. with CrO 3 , DCC/DMS, SO 3 /py, Br 2 /LiBr/Li 2 CO 3 /DMF or with Al(OPr i ) 3 or Al(OBu t ) 3 optionally in the presence of DDQ; or (b) from the corresponding # 5(10) or # 5(10) , 16 -3- ones by acid or base # 5(10) ## 4 isomerization; and are interconvertible by chemical or microbial 1,2- and/or 6,7-dehydrogenation. Compounds I (R 7 is other than H) are prepared from the corresponding 6,7-dehydro compounds (where R 7 =H) by reacting with H 2 S, a mercaptan or a thiocarboxylic acid, optionally followed by 1,2-dehydrogenation. The starting materials are prepared as described in Specifications 1,450,885 and 1,450,886. Compounds I are said to affect body mineral reserves, and may be made up with carriers into pharmaceutical compositions for oral, parenteral rectal and topical administration.

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