WO2003004515A1 - Process for production of estradiol derivatives, intermediates used in the process and process for production thereof - Google Patents

Process for production of estradiol derivatives, intermediates used in the process and process for production thereof 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
French (fr)
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/en
Publication of WO2003004515A1 publication Critical patent/WO2003004515A1/en

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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)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The invention aims at providing a process for industrial production of novel estradiol derivatives useful as drugs; intermediates used in the process; and a process for production of the intermediates. The invention provides a process for production of compounds represented by the general formula (|): (|) (wherein m is an integer of 2 to 14; n is an integer of 2 to 7; and R4 is linear or branched halogenoalkyl having 1 to 7 carbon atoms), which comprises the step of introducing a side chain represented by the general formula: -(CH2)mCH(COOR3)-(CH2)n-R4 (wherein m, n, and R4 are each as defined above; and R3 is a carboxyl-protecting group) to the 7-position of a compound represented by the general formula (||): (||) (wherein R1 and R2 are each independently a hydroxyl-protecting group), and the step of conducting reduction of the carbonyl group at the 6-position and deblocking of the hydroxyl-protecting groups at the 3- and 17-positions and the carboxyl-protecting group.
PCT/JP2002/006896 2001-07-06 2002-07-08 Process for production of estradiol derivatives, intermediates used in the process and process for production thereof WO2003004515A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2003510681A JPWO2003004515A1 (en) 2001-07-06 2002-07-08 Method for producing estradiol derivative, intermediate used in the method and method for producing the same

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 (en) 2003-01-16

Family

ID=19043061

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/006896 WO2003004515A1 (en) 2001-07-06 2002-07-08 Process for production of estradiol derivatives, intermediates used in the process and process for production thereof

Country Status (2)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003087120A1 (en) * 2002-04-02 2003-10-23 Chugai Seiyaku Kabushiki Kaisha Estrone derivative and process for producing the same
WO2017170036A1 (en) * 2016-03-31 2017-10-05 富士フイルム株式会社 Colored composition, light-absorbing anisotropic film, layered product, and image display device

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59110675A (en) * 1982-12-16 1984-06-26 Ss Pharmaceut Co Ltd Pyridine derivative and its preparation
WO1997024387A1 (en) * 1995-12-29 1997-07-10 Minnesota Mining And Manufacturing Company Fluorine containing poly (beta-hydroxyorganoate)
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 (en) * 1999-12-13 2001-06-14 Chugai Seiyaku Kabushiki Kaisha Compound having hydroxycarbonyl-halogenoalkyl side chain
WO2001060836A1 (en) * 2000-02-18 2001-08-23 Taiho Pharmaceutical Co., Ltd. Process for the preparation of steroid derivatives

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59110675A (en) * 1982-12-16 1984-06-26 Ss Pharmaceut Co Ltd Pyridine derivative and its preparation
WO1997024387A1 (en) * 1995-12-29 1997-07-10 Minnesota Mining And Manufacturing Company Fluorine containing poly (beta-hydroxyorganoate)
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 (en) * 1999-12-13 2001-06-14 Chugai Seiyaku Kabushiki Kaisha Compound having hydroxycarbonyl-halogenoalkyl side chain
WO2001060836A1 (en) * 2000-02-18 2001-08-23 Taiho Pharmaceutical Co., Ltd. Process for the preparation of steroid derivatives

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 (en) * 2002-04-02 2003-10-23 Chugai Seiyaku Kabushiki Kaisha Estrone derivative and process for producing the same
WO2017170036A1 (en) * 2016-03-31 2017-10-05 富士フイルム株式会社 Colored composition, light-absorbing anisotropic film, layered product, and image display device
JPWO2017170036A1 (en) * 2016-03-31 2019-02-28 富士フイルム株式会社 Coloring composition, light-absorbing anisotropic film, laminate and image display device

Also Published As

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

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