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    PROCESS FOR THE PREPARATION OF 3ß-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)ANDROSTA-5,16-DIENE
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF 3ß-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)ANDROSTA-5,16-DIENE 审中-公开
    制备3β-羟基-17-（1H-苯并咪唑-1-基）ANDROSTA-5,16-二烯的方法

    公开(公告)号：WO2018029223A1

    公开(公告)日：2018-02-15

    申请号：PCT/EP2017/070124

    申请日：2017-08-08

    Applicant: INDUSTRIALE CHIMICA S.R.L.

    Inventor： BARBIERI, Francesco ,  LENNA, Roberto

    IPC: C07J43/00

    Abstract: A process for the synthesis of β-hydroxy 3-17-(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 (6).

    Abstract translation: 描述了一种合成β-羟基3-17-（1H-苯并咪唑-1-基）雄甾-5,16-二烯的方法，该化合物也称为Galeterone并用于 治疗前列腺癌，具有公式（6）。

    PROCESS FOR THE PREPARATION OF DROSPIRENONE AS A FINE POWDER THROUGH A DOUBLE CHANGE OF CRYSTALLINE FORM
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF DROSPIRENONE AS A FINE POWDER THROUGH A DOUBLE CHANGE OF CRYSTALLINE FORM 审中-公开

    公开(公告)号：WO2022215048A1

    公开(公告)日：2022-10-13

    申请号：PCT/IB2022/053322

    申请日：2022-04-08

    Applicant: INDUSTRIALE CHIMICA S.R.L.

    Inventor： LENNA, Roberto ,  BALDRIGHI, Michele

    IPC: C07J53/00 ,  A61P5/00

    Abstract: The present invention refers to a process for the industrial-scale preparation of 17β-hydroxy- 6β,7β;15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid y-lactone, known by the common name of Drospirenone, in the form of a fine powder without the use of mechanical grinding or micronization techniques, but rather exploiting a double change of crystalline form, from Crystalline Form I to Crystalline Form II and from Crystalline Form II to Crystalline Form I. The invention also refers to the new Crystalline Form II of Drospirenone obtained in the process.

    PROCESS FOR THE PREPARATION OF ABIRATERONE OR ABIRATERONE ACETATE
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF ABIRATERONE OR ABIRATERONE ACETATE 审中-公开
    制备阿维菌素或乙酸阿贝特龙的方法

    公开(公告)号：WO2015014686A1

    公开(公告)日：2015-02-05

    申请号：PCT/EP2014/065813

    申请日：2014-07-23

    Applicant: INDUSTRIALE CHIMICA S.R.L.

    Inventor： LENNA, Roberto ,  DI BRISCO, Riccardo

    IPC: C07J31/00 ,  C07J43/00

    CPC classification number: C07J43/003 ,  C07J31/006

    Abstract: The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression of advanced stage prostate cancer. The process is characaterised by the fact that the intermediate triflation step is carried out on prasterone (DHEA) or its 3-acetate using Ar-N(OTf) 2 as the triflation reagent, but where Ar is not phenyl, and by the fact that the base used in this step is an alkali metal alcoholate.

    Abstract translation: 本发明涉及一种用于合成阿维酮酮，特别是阿维昔龙醋酸酯的新方法，该方法报告如下：具有适于减缓晚期前列腺癌进展的药理学活性。 该方法的特征在于以下事实：中间三价充气步骤使用Ar-N（OTf）2作为三氟化试剂进行prasterone（DHEA）或其3-乙酸酯，但是Ar不是苯基，而事实上 该步骤中使用的碱是碱金属醇化物。

    PROCESS FOR THE PREPARATION OF ABIRATERONE AND ABIRATERONE ACETATE
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF ABIRATERONE AND ABIRATERONE ACETATE 审中-公开
    制备阿片类和乙酰丙酸酯的方法

    公开(公告)号：WO2015015246A1

    公开(公告)日：2015-02-05

    申请号：PCT/IB2013/056206

    申请日：2013-07-29

    Applicant: INDUSTRIALE CHIMICA S.R.L.

    Inventor： LENNA, Roberto ,  DI BRISCO, Riccardo

    IPC: C07J31/00 ,  C07J43/00

    CPC classification number: C07J43/003 ,  C07J31/006

    Abstract: The present invention relates to a novel process for the synthesis of abiraterone, and in particular of abiraterone acetate, compound of formula (I) reported below: N O (I) which has pharmacological activity useful tor slowing down the progression of prostate cancer at an advanced stage. The process is characterised by an intermediate step wherein DHEA-acetate is triflated using Ar-N(OTf) 2 as the triflation reagent.

    Abstract translation: 本发明涉及一种用于合成阿维酮酮的新方法，特别是乙酸阿比酮酮，如下所述的式（I）化合物：具有药理学活性的NO（I）可用于降低前列腺癌进展的进展 阶段。 该方法的特征在于其中使用Ar-N（OTf）2作为三氟化试剂使DHEA-乙酸酯进行三氟甲磺酸酯化的中间步骤。

    PROCESS FOR THE PREPARATION OF DROSPIRENONE
    8.
    发明申请
    PROCESS FOR THE PREPARATION OF DROSPIRENONE 审中-公开
    制备吡罗昔酮的方法

    公开(公告)号：WO2006061309A1

    公开(公告)日：2006-06-15

    申请号：PCT/EP2005/055963

    申请日：2005-11-14

    Applicant: INDUSTRIALE CHIMICA S.R.L. ,  COSTANTINO, Francesca ,  LENNA, Roberto ,  PIURI, Silvia

    Inventor： COSTANTINO, Francesca ,  LENNA, Roberto ,  PIURI, Silvia

    IPC: C07J53/00 ,  A61K31/585 ,  A61P15/18

    CPC classification number: C07J53/008

    Abstract: A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action; comprising the oxidation of 17α-(3-hydroxypropyl)-6β, 7β, 15β, 16β-dimethylene-5β-androstane- 3β , 5, 17β -triol.

    Abstract translation: 描述了制备屈螺酮的方法，屈螺酮是具有孕激素，抗皮质激素和抗雄激素活性的合成类固醇，可用于制备具有避孕作用的药物组合物; 包括17a-（3-羟丙基）-6β，7β，15β，16β-二亚甲基-5β-雄甾烷-3β，5β，17β-三醇的氧化。

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