WO2003004515A1 - Procede de production de derives d'estradiol, produits intermediaires utilises dans ce procede et procede de production de ces derniers - Google Patents

Procede de production de derives d'estradiol, produits intermediaires utilises dans ce procede et procede de production de ces derniers Download PDF

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Publication number
WO2003004515A1
WO2003004515A1 PCT/JP2002/006896 JP0206896W WO03004515A1 WO 2003004515 A1 WO2003004515 A1 WO 2003004515A1 JP 0206896 W JP0206896 W JP 0206896W WO 03004515 A1 WO03004515 A1 WO 03004515A1
Authority
WO
WIPO (PCT)
Prior art keywords
production
general formula
protecting group
intermediates used
estradiol derivatives
Prior art date
Application number
PCT/JP2002/006896
Other languages
English (en)
Japanese (ja)
Inventor
Yukio Suzuki
Tatsuya Kato
Hiroshi Aoyama
Tomoko Misono
Khlebnikov A Vladimir
Akemi Mizutani
Yoshihito Ohtake
Takuma Ikeda
Koji Takano
Heean Kwon
Pil-Su Ho
Ju-Su Kim
Won-Il Lee
Chan-Hee Park
Sang-Hak Lee
Sung-Oh Ahn
Original Assignee
Chugai Seiyaku Kabushiki Kaisha
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chugai Seiyaku Kabushiki Kaisha filed Critical Chugai Seiyaku Kabushiki Kaisha
Priority to JP2003510681A priority Critical patent/JPWO2003004515A1/ja
Publication of WO2003004515A1 publication Critical patent/WO2003004515A1/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)

Abstract

La présente invention a pour objet un procédé de production industrielle de nouveaux dérivés d'estradiol utiles comme médicaments ; des produits intermédiaires utilisés dans ce procédé et un procédé de production de ces derniers. La présente invention concerne un procédé de production de composés représentés par la formule générale (I). Dans cette dernière m est un nombre entier compris entre 2 et 14 ; n est un nombre entier compris entre 2 et 7 ; et R4 est un halogénoalkyl ramifié ou linéaire avec 1 à 7 atomes de carbone. Ce procédé comprend les étapes consistant à introduire une chaîne latérale représentée par la formule générale (CH¿2?),CH(COOR?3)-(CH¿2)n-R4 (où m, n et R4 sont chacun définis comme ci-dessus ; et R3 est un groupe protecteur carboxyl) à la position 7 d'un composé représenté par la formule générale (II). Dans cette dernière R1 et R2 sont chacun un groupe protecteur hydroxyl. Ce procédé comprend l'étape consistant à réduire le groupe carbonyle à la position 6 et débloquer les groupes protecteurs hydroxyle aux positions 3 et 17 et le groupe protecteur carboxyl.
PCT/JP2002/006896 2001-07-06 2002-07-08 Procede de production de derives d'estradiol, produits intermediaires utilises dans ce procede et procede de production de ces derniers WO2003004515A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2003510681A JPWO2003004515A1 (ja) 2001-07-06 2002-07-08 エストラジオール誘導体の製造方法、当該方法で用いる中間体及びその製造方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2001-207013 2001-07-06
JP2001207013 2001-07-06

Publications (1)

Publication Number Publication Date
WO2003004515A1 true WO2003004515A1 (fr) 2003-01-16

Family

ID=19043061

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/006896 WO2003004515A1 (fr) 2001-07-06 2002-07-08 Procede de production de derives d'estradiol, produits intermediaires utilises dans ce procede et procede de production de ces derniers

Country Status (2)

Country Link
JP (1) JPWO2003004515A1 (fr)
WO (1) WO2003004515A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003087120A1 (fr) * 2002-04-02 2003-10-23 Chugai Seiyaku Kabushiki Kaisha Derive d'oestrone et procede de production dudit derive
WO2017170036A1 (fr) * 2016-03-31 2017-10-05 富士フイルム株式会社 Composition colorée, film anisotrope absorbant la lumière, produit stratifié, et dispositif d'affichage d'image

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59110675A (ja) * 1982-12-16 1984-06-26 Ss Pharmaceut Co Ltd ピリジン誘導体及びその製造方法
WO1997024387A1 (fr) * 1995-12-29 1997-07-10 Minnesota Mining And Manufacturing Company Poly (beta-hydroxyorganoates) fluores
US5902888A (en) * 1997-11-14 1999-05-11 Bayer Corporation Synthesis of 6α-functionalized estriol haptens and protein conjugates thereof
US6136992A (en) * 1997-03-13 2000-10-24 The United States Of America As Represented By The Department Of Health And Human Services 2-alkoxy estradiols and derivatives thereof
WO2001042186A1 (fr) * 1999-12-13 2001-06-14 Chugai Seiyaku Kabushiki Kaisha Compose a chaine laterale hydroxycarbonyl-halogenoalkyle
WO2001060836A1 (fr) * 2000-02-18 2001-08-23 Taiho Pharmaceutical Co., Ltd. Procede de preparation de derives steroidiens

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59110675A (ja) * 1982-12-16 1984-06-26 Ss Pharmaceut Co Ltd ピリジン誘導体及びその製造方法
WO1997024387A1 (fr) * 1995-12-29 1997-07-10 Minnesota Mining And Manufacturing Company Poly (beta-hydroxyorganoates) fluores
US6136992A (en) * 1997-03-13 2000-10-24 The United States Of America As Represented By The Department Of Health And Human Services 2-alkoxy estradiols and derivatives thereof
US5902888A (en) * 1997-11-14 1999-05-11 Bayer Corporation Synthesis of 6α-functionalized estriol haptens and protein conjugates thereof
WO2001042186A1 (fr) * 1999-12-13 2001-06-14 Chugai Seiyaku Kabushiki Kaisha Compose a chaine laterale hydroxycarbonyl-halogenoalkyle
WO2001060836A1 (fr) * 2000-02-18 2001-08-23 Taiho Pharmaceutical Co., Ltd. Procede de preparation de derives steroidiens

Non-Patent Citations (17)

* Cited by examiner, † Cited by third party
Title
ARZNEIM. FORSCH., vol. 33, no. 3, 1983, pages 347 - 352, XP002957823 *
CHEM. PHYS. LIPIDS, vol. 79, no. 1, 1996, pages 71 - 77, XP002957821 *
CHEMICAL ABSTRACTS, vol. 115, Columbus, Ohio, US; abstract no. 256478, XP002958152 *
CHEMICAL ABSTRACTS, vol. 74, Columbus, Ohio, US; abstract no. 22273, XP002958153 *
J. AM. CHEM. SOC., vol. 102, no. 8, 1980, pages 2693 - 2698, XP002957818 *
J. CHEM. SOC., PERKIN TRANS. 1, no. 10, 1993, pages 1183 - 1189, XP002957820 *
J. LABELLED COMP. RADIOPHARM., vol. 43, no. 13, 2000, pages 1289 - 1300, XP002957815 *
J. ORG. CHEM., vol. 35, no. 12, 1970, pages 4241 - 4244 *
J. ORG. CHEM., vol. 47, no. 2, 1982, pages 222 - 226, XP002957816 *
J. ORG. CHEM., vol. 58, no. 10, 1993, pages 2910 - 2912, XP002957822 *
LIEBIGS ANN. CHEM., no. 8, 1989, pages 719 - 726, XP002957817 *
LIQUID CRYSTALS, vol. 19, no. 6, 1995, pages 759 - 764, XP000554518 *
NEW. J. CHEM., vol. 15, no. 8-9, 1991, pages 685 - 692 *
STEROIDS, vol. 65, no. 9, 2000, pages 497 - 504, XP004209376 *
SYNTHESIS, no. 12, 1995, pages 1493 - 1495, XP002957824 *
TETRAHEDRON LETT., vol. 31, no. 15, 1990, pages 2161 - 2164, XP002957819 *
TETRAHEDRON LETTERS, vol. 38, no. 18, 1997, pages 3171 - 3174, XP004059799 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003087120A1 (fr) * 2002-04-02 2003-10-23 Chugai Seiyaku Kabushiki Kaisha Derive d'oestrone et procede de production dudit derive
WO2017170036A1 (fr) * 2016-03-31 2017-10-05 富士フイルム株式会社 Composition colorée, film anisotrope absorbant la lumière, produit stratifié, et dispositif d'affichage d'image
JPWO2017170036A1 (ja) * 2016-03-31 2019-02-28 富士フイルム株式会社 着色組成物、光吸収異方性膜、積層体および画像表示装置

Also Published As

Publication number Publication date
JPWO2003004515A1 (ja) 2004-10-28

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