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    PROCESS FOR PREPARING 16'alpha'-HYDROXY-ESTRA-1,3,5(10)-TRIENE DERIVATIVES
    5.
    发明申请
    PROCESS FOR PREPARING 16'alpha'-HYDROXY-ESTRA-1,3,5(10)-TRIENE DERIVATIVES 审中-公开
    PROCESS FOR 16的α-羟基 - 雌甾-1,3,5（10） - 三烯衍生物的制备

    公开(公告)号：WO1998004577A1

    公开(公告)日：1998-02-05

    申请号：PCT/EP1997003708

    申请日：1997-07-11

    Applicant: SCHERING AG ,  HÄUSER, Helmut ,  MEYER, Michael ,  RAMIREZ, Daniel ,  MORALES, Manuel

    Inventor： SCHERING AG

    IPC: C07J01/00

    CPC classification number: C07J1/007 ,  C07J1/0059 ,  C07J13/005 ,  C07J71/001

    Abstract: A process is disclosed for preparing 16 alpha -hydroxy-estra-1,3,5(10)-triene derivatives having the general formula (I), in which R1 stands for a hydrogen atom, an alkyl group with maximum 4 carbon atoms, a benzyl group or an acyl group with maximum 8 carbon atoms; and X and Y represent together an oxo group or X stands for a hydroxyl group and Y for a hydrogen atom. This process is characterised in that an estra-1,3,5(10),16-tetraene derivative is converted by means of peracids into a 16 alpha ,17 alpha -epoxide, which is split by means of mineral acids or converted by means of a reagent which supplies bromine cations into the corresponding 16 alpha -bromine derivative, which is converted into the 16 beta -bromine derivative. The bromine is replaced by an hydroxyl group and if required the thus obtained 16 alpha -hydroxy-1,3,5(10)triene-17-one derivative is reduced by means of sodium hydroboron in the presence of a strong aqueous buffer solution with a pH value from 5 to 6.5 into the corresponding 16 alpha ,17 beta -trihydroxy-estra-1,3,5(10)-triene derivative.

    Abstract translation: 本发明涉及一种方法，用于制备16α-羟基 - 雌-1,3,5（10）通式（I）其中R1是氢原子，具有至多4个碳原子，苄基或一个烷基基团的 - 三烯衍生物 是指具有至多8个碳原子的酰基，X和Y一起表示氧基或其中X是羟基和Y表示氢原子，其特征在于，雌甾-1,3,5（10），16-四烯衍生物装置 过酸通过由在ensprechende 16的α-溴代衍生物溴阳离子试剂转移的装置提供无机酸装置转移到16α，17的α-环氧化物，而这种分割或，这对于16重排的β-溴代衍生物，然后抵靠溴 取代的羟基，然后选择性地将得到的16α-羟基-1,3,5（10）三烯-17-酮在pH为5的一个强有力的缓冲水溶液的存在下衍生物6.5借助于Natriumborh ydrid到相应的16α，17的β三羟基降低 - 雌-1,3,5（10） - 三烯衍生物。

    17-SUBSTITUTED STEROIDS USEFUL IN CANCER TREATMENT
    7.
    发明申请
    17-SUBSTITUTED STEROIDS USEFUL IN CANCER TREATMENT 审中-公开
    17-替代的甾体有用于癌症治疗

    公开(公告)号：WO1993020097A1

    公开(公告)日：1993-10-14

    申请号：PCT/GB1993000531

    申请日：1993-03-15

    Applicant: BRITISH TECHNOLOGY GROUP LTD. ,  BARRIE, Susan, Elaine ,  JARMAN, Michael ,  POTTER, Gerard, Andrew

    Inventor： BRITISH TECHNOLOGY GROUP LTD.

    IPC: C07J43/00

    CPC classification number: C07J13/005 ,  C07J31/006 ,  C07J41/0005 ,  C07J43/003 ,  C07J51/00

    Abstract: Compounds of general formula (1) wherein X represents the residue of the A, B and C rings of a steroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R14 represents a hydrogen atom and R15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R?14 and R15¿ together represent a double bond, and R16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or pharmaceutically acceptable acid addition salts, with the proviso that 17-(3-pyridyl)androsta-5,14,16-trien-3β-ol and 15β-acetoxy-17-(3-pyridyl)androsta-5,16-dien-3β-ol and their 3-acetates and 3β-methoxy-17-(3-pyridyl)androst-16-ene are claimed only for use in therapy are useful for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.

    11'beta'-SUBSTITUTED PROGESTERONE ANALOGS
    8.
    发明申请
    11'beta'-SUBSTITUTED PROGESTERONE ANALOGS 审中-公开
    11 beta - 发酵的孕激素类似物

    公开(公告)号：WO1989012448A1

    公开(公告)日：1989-12-28

    申请号：PCT/US1989002706

    申请日：1989-06-23

    Applicant: RESEARCH TRIANGLE INSTITUTE

    Inventor： RESEARCH TRIANGLE INSTITUTE ,  COOK, C., Edgar ,  WANI, Mansukh, C. ,  LEE, Yue-Wei ,  REEL, Jerry, R. ,  RECTOR, Douglas

    IPC: A61K31/56

    CPC classification number: C07J41/0083 ,  C07J7/002 ,  C07J7/0045 ,  C07J13/005 ,  C07J53/004 ,  C07J71/0052

    Abstract: An 11 beta -aryl-19-norprogesterone steroid of formula (I): wherein (i) R is H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, OH, OC(O)CH3, or OC(O)R , wherein R is C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl or aryl, R2 is H, R is H, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl, R is H, CH3, F or Cl, R is H, (CH3)2N, CH3O, CH3CO, CH3S, CH3SO, CH3SO2, and X is O or NOCH3; or (ii) R and R taken together are a carbon-carbon bond and R , R , R and X are as defined above; or (iii) R and R taken together are -CH2- or -N=N-CH2-, R is H and R , R and X are as defined above; or (iv) R and R taken together are =CH2 and R , R , R and X are as defined above.

    Abstract translation: 式（I）的11β-芳基-19-去甲孕酮类固醇：其中（i）R 1是H，C 1-4烷基，C 2-4烯基，C 2-4炔基，OH，OC（O）CH 3， 或OC（O）R 5，其中R 5是C 2-8烷基，C 2-8烯基，C 2-8炔基或芳基，R 2是H，R 3是H，C 1-4烷基，C 2 -4-烯基或C 2-4炔基，R 4是H，CH 3，F或Cl，R 6是H，（CH 3）2 N，CH 3 O，CH 3 CO，CH 3 S，CH 3 SO，CH 3 SO 2，X是O或NOCH 3 ; 或（ii）R 1和R 2一起是碳 - 碳键，R 3，R 4，R 6和X如上所定义; 或（iii）R 1和R 3一起是-CH 2 - 或-N = N-CH 2 - ，R 2是H且R 4，R 6和X如上所定义 ; 或（iv）R 2和R 3一起为= CH 2且R 1，R 4，R 6和X如上所定义。

    PROCESS FOR THE PREPARATION OF GALETERONE
    10.
    发明申请
    PROCESS FOR THE PREPARATION OF GALETERONE 审中-公开
    制备GALETERONE的方法

    公开(公告)号：WO2017208132A1

    公开(公告)日：2017-12-07

    申请号：PCT/IB2017/053147

    申请日：2017-05-29

    Applicant: INDUSTRIALE CHIMICA S.R.L.

    Inventor： BARBIERI, Francesco ,  LENNA, Roberto

    IPC: C07J43/00 ,  C07J75/00

    CPC classification number: C07J43/003 ,  C07J1/0011 ,  C07J13/005

    Abstract: A process for the synthesis of 3β-hydroxy-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (I) given below.

    Abstract translation: 描述了一种合成3β-羟基-17-（1H-苯并咪唑-1-基）雄甾-5,16-二烯的方法，该化合物也被称为Galeterone并用于治疗 具有下面给出的式（I）的前列腺癌。

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