NEW STEROID HAVING METHYLENE LACTONE GROUP ON 17-TH POSITION, ITS PRODUCTION, ITS INTERMEDIATE, ITS USE AS PHARMACEUTIC, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

Title:

NEW STEROID HAVING METHYLENE LACTONE GROUP ON 17-TH POSITION, ITS PRODUCTION, ITS INTERMEDIATE, ITS USE AS PHARMACEUTIC, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

Document Type and Number:

Japanese Patent JP3466651

Kind Code:

B2

Abstract:

PURPOSE: To obtain a new steroid which contains a methylene lactone group on 17-th position, which shows various hormonal activities and antihormonal activities and which is useful as a therapeutic drug for prostatic hyperfrophy, virilism, polytrichia, prostate cancer, breast cancer, lung cancer or the like.
CONSTITUTION: A compd. expressed by formula I is reacted with a compd. expressed by formula II to obtain a compd. expressed by formula III comprising a mixture of isomers on 17-th position. In formula I, R1p, is a group R1 in which allowable reactive functional groups may be protected, (R1 is phenyl, biphenyl, thienyl, furyl or the like which may be substd.); R2 is a 1-4C alkyl on α or β position; K is a blocked ketone. In formula II, Hal is a halogen; Alk is a 1-4C 1lkyl. Then, a dehydrating agent which can open ketone functional groups is reacted with the compd. of formula III, and then the protecting groups which the R1, group may contain are removed. Further, an agent to produce aromatic groups, a saponifying agent and an alkylating or acylating agent are allowed to react to obtain salts of a compd. expressed by formula IV with an acid and a base. In formula IV, A, B are expressed by formula V, formula VI. (Rd is H, a 1-4C alkyl or the like.).

Inventors:

Lucian Nedlek
Francois Neek
Daniel Philibert

Application Number:

JP6127793A

Publication Date:

November 17, 2003

Filing Date:

February 26, 1993

Export Citation:

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Assignee:

Aventis Pharma Societe Anonym

International Classes:

A61P3/10; A61P5/24; A61P5/36; A61P9/08; A61P9/12; A61P13/02; A61P15/00; A61P19/10; A61P25/04; A61P25/20; A61P37/04; A61K31/585; C07J1/00; C07J21/00; C07J31/00; C07J41/00; (IPC1-7): C07J21/00; A61K31/585; A61P3/10; A61P5/24; A61P5/36; A61P9/08; A61P9/12; A61P15/00; A61P19/10; A61P25/20; A61P37/04

Attorney, Agent or Firm:

Motohiro Kurauchi (1 outside)

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