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    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID
    1.
    发明授权
    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID 失效

    公开(公告)号：KR800000809B1

    公开(公告)日：1980-08-21

    申请号：KR750002179

    申请日：1975-10-07

    Applicant: HOFFMANN LA ROCHE

    Inventor： MULLER M ,  WEICHERT R ,  KERB U ,  ALIG L

    IPC: C07J63/00

    Abstract: D-homosteroid(I;R6=H, F, Cl, methyl;R17a=hydroxy, acyloxy, alkoxy, lower alkyl; R21=H, F, Cl), having progestational activity, was prepd, by oxidation of compd. II. Thus, 1.15 g 3β-hydroxy-17aα-methyl-D-homo-5, 16-pregnadiene-20-one and a mixt. of 1.1 ml cyclohexano and 22 m1 toluene were boiled, and added 550 mg aluminium isopropylate and 2 ml toluene, destillated for 45 min to give 17aα-methyl-D-homo-4, 16-pregnadiene-3, 20-dione(m.p.181.5- ! 185.5≦̸C).

    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID
    2.
    发明授权
    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID 失效

    公开(公告)号：KR800000812B1

    公开(公告)日：1980-08-21

    申请号：KR790003615

    申请日：1979-10-19

    Applicant: HOFFMANN LA ROCHE

    Inventor： MULLER M ,  WEICHERT R ,  KERB U ,  ALIG L

    IPC: C07J63/00

    Abstract: D-Homosteroids [R1, R2=H or 1α, 2α-methylene, C-C; R6=H, F, Cl, Me; R17a=OH, acyloxy, alkoxy, lower alkyl; R10=Me or H when R1, R2 is H; R21=F, Cl) having hormonal activity esp. on topmarked anti-inflammatory effect were prepd. by reacting compd. II with CClO4 or triphenyl phosphin in the dimethyl formamide.

    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS
    3.
    发明授权
    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS 失效

    公开(公告)号：KR800000406B1

    公开(公告)日：1980-05-20

    申请号：KR790002866

    申请日：1979-08-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： MULLER M ,  ALIG L ,  FURST A

    IPC: C07J63/00

    Abstract: D-homosteroids(I, R6 = H, F, Cl, Br, methyl; R11 = F, Cl, hydroxy; R9 = H, F, Cl, Br; R21 = residue group of sulfate or phosphate, aq. salt of carboxylic acid, acyloxy; R17a = hydroxy, acyloxy) useful as anti-inflammatory agent, were prepd. by reaction of D-homosteroid(II, R201 = hydroxymethyl, halomethyl) and sulfate or phosphate in the presence of acylating agent. Thus, 11β,17a-dihydroxy-21,21-diiodo-D-homopreg-4-ene-3,20-dione was dissolved in acetone, following by reaction with H2O K2HPO4 and o-phosphoric acid. The reaction product was rdfluxed in dark place to give I.

    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID
    4.
    发明授权
    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID 失效

    公开(公告)号：KR800000810B1

    公开(公告)日：1980-08-21

    申请号：KR750002257

    申请日：1975-10-17

    Applicant: HOFFMANN LA ROCHE

    Inventor： MULLER M ,  WEICHERT R ,  KERB U ,  ALIG L

    IPC: C07J63/00

    Abstract: Title compds. (I;R3=oxo;R13=lower alkyl, R17β=H,acyl, lower alkyl;R17aα=H, lower alkyl, ethinyl, vinyl, l, propinyl, chloroethinyl, butadienyl, propadienyl;The dotted line in ring A means additive C-C bond at 4,5-or 5(10)-position) are prepd. by hydrolysing compd. II(R13=group changed to 3-keto-Δ3 or 3-keto-Δ5(10) group by hydrolysis) with inoraganic acid or carboxylic acid in alcohol-H2O mixt. The final products exhibit hormanal action such as suppression of pregnancy or ovulation.

    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS
    5.
    发明授权
    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS 失效

    公开(公告)号：KR800000405B1

    公开(公告)日：1980-05-20

    申请号：KR790002865

    申请日：1979-08-22

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURST A ,  ALIG L ,  MULLER M

    IPC: C07J63/00

    Abstract: D-homosteroids(I, R6 = H, F, Cl, Br, Me; R11 = F, Cl, OH; R17a= OH, acyloxy) useful as anti-inflammatory agent, were prepd. by halogenating 21-position of compd. II(R20 =Me, MeOH). Thus, 590mg 9-fluoro-11β, 17a, 21-trihyihydroxy-D-homopregna-1,4-diene-3, 20-dione and 590mg triphenylphosphine were dissolved in 6ml DMF, and added 0.5ml CCl4. The mixt. was treated for 1 hr, and extracted to give 405ml 21-chloro-9-fluoro-11β, 17a-dihydroxy-D- homopregna-1,4-diene-30,20-dione.

    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID
    6.
    发明授权
    PROCESS FOR THE PREPARATION OF D-HOMOSTEROID 失效

    公开(公告)号：KR800000811B1

    公开(公告)日：1980-08-21

    申请号：KR790003614

    申请日：1979-10-19

    Applicant: HOFFMANN LA ROCHE

    Inventor： MULLER M ,  WEICHERT R ,  KERB U ,  ALIG L

    IPC: C07J63/00

    Abstract: The title compds. (I; R17a=hydroxy, acyloxy, lower alkyl; R21=H, F, Cl) with hormonal action were prepd. by multistep synthesis. Key steps include the hydrolysing of compd. II(X=alkoxy, alkylthio, sec-amino, alkylenedioxy, alkylenedithio) and fluorinating or chlorinating at C6 position, if necessary, and methylating at C6 position or acylating hydroxyl group.

    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS
    7.
    发明授权
    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS 失效

    公开(公告)号：KR800000407B1

    公开(公告)日：1980-05-20

    申请号：KR740003675

    申请日：1974-09-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURST A ,  ALIG L ,  MULLER M

    IPC: C07J63/00

    Abstract: D-homosteroids(I, R6 = H, F, Cl, Br, Me; R11 = hydroxy, F, Cl, R9 = F, Cl, Br; R21 = halogen, acyloxy, R; R =residue group of sulfate, phosphate, or water-sol. salt of di- or tricarboxylic acid; R17a = hydroxy, acyloxy), useful as anti-inflammatory agent, were prepd. by addition of halogen in 9,11double bond position of compd.II. Thus, 21-acetoxy-17a-hydroxy-D- homopregna-4,9(11)-diene-3,20-dione was dissolved in chloroform, and reacted with Cl-satd. CCl4 for 1 hr to give 21-acetoxy-9α-11β-dichloro-17a-hydroxy-D-homopr eg-4-ene-3, 20-dione..

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