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    PROCESS FOR PREPARATION OF D-HOMOSTEROIDS
    1.
    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 PREPARATION OF D-HOMOSTEROIDS
    2.
    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..

    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.

    20-hydrocarbyl-6-keto-steroids
    5.
    发明授权
    20-hydrocarbyl-6-keto-steroids 失效
    20-油酰六-KETO-STEROIDS

    公开(公告)号：US3835127A

    公开(公告)日：1974-09-10

    申请号：US70923968

    申请日：1968-02-29

    Applicant: HOFFMANN LA ROCHE

    Inventor： FURST A ,  FURLENMEIER A ,  WIECHERT R ,  HOCKS P ,  KERB U ,  LANGEMANN A ,  WALDVOGEL G

    IPC: C07J9/00 ,  C07C173/00

    CPC classification number: C07J9/00

    Abstract: This invention is directed to 2,3-substituted-20-hydrocarbyl 6keto-steroids which are useful as metamorphosis hormones and are additionally useful as intermediates for the production of other insect hormones. Accordingly, the compounds may be employed in the control of insect population.

    Abstract translation: 本发明涉及可用作变态激素的2,3-取代的20-烃基6-酮类固醇，并且还可用作生产其它昆虫激素的中间体。 因此，这些化合物可用于防治昆虫群体。

    Retrosteroid a ring formation
    7.
    发明授权
    Retrosteroid a ring formation 失效
    回归环形成

    公开(公告)号：US3766213A

    公开(公告)日：1973-10-16

    申请号：US3766213D

    申请日：1971-01-06

    Applicant: HOFFMANN LA ROCHE

    Inventor： USKOKOVIC M ,  FURST A ,  KOCH W

    IPC: C07C59/205 ,  C07C59/215 ,  C07D7/26

    CPC classification number: C07C59/205 ,  C07C59/215 ,  C07C2603/16 ,  C07J15/005 ,  C07J75/005

    Abstract: A PROCESS FOR PRODUCING KNOWN RETROSTEROIDS OF THE FORMULA:

    1-R1,2-R2,3-(O=),4-R4,6-R6,7-R7,11-R11,16-R16-ANDROST-4-

    ENE WHERE C17 IS Z

    WHEREIN: R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R2 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R6 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER AKLANOYLTHIO, AND HALO; R7 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO, AND HALO; R11 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY AND LOWER ALKANOYLOXY; R16 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, HYDROXY, LOWER ALKOXY, LOWER ALKANOYLOXY, AND, WHEN THE 17B-SUBSTITUENT IS ACETYL OR SUBSTITUTED ACETYL, FLUORINE; Z IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF CARBONYL, (17B-HYDROXY-17-A-LOWER ALKANOIC ACID LACTONE), AND

    >C(-R17ALPHA)-R17BETA

    R17B IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, LOWER ALKANOYLOXY, AND

    Y-CH2-CO-

    Y IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALO, AND HYDROXY; R17A, WHEN R17B IS HYDROXY AND LOWER ALKANOYLOXY, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALIPHATIC HYDROCARBYL, AND WHEN R17B IS

    Y-CH2-CO-

    IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN ALKYL, HYDROXY, LOWER ALKANOYLOXY, AND HALO; Q WHEN TAKEN ALONE, IS OXO; T1 WHEN TAKEN ALONE, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKALI METAL OXY AND LOWER ALKOXY; AND T1 AND Q, WHEN TAKEN TOGETHER ARE NITROLO.

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