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WO2002042261A3 - PROCESS FOR PREPARING α-(3-ARYLTHIO)-ACETOPHENONES - Google Patents

PROCESS FOR PREPARING α-(3-ARYLTHIO)-ACETOPHENONES Download PDF

Info

Publication number
WO2002042261A3
WO2002042261A3 PCT/US2001/042939 US0142939W WO0242261A3 WO 2002042261 A3 WO2002042261 A3 WO 2002042261A3 US 0142939 W US0142939 W US 0142939W WO 0242261 A3 WO0242261 A3 WO 0242261A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparing
acetophenones
arylthio
compound
formula
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2001/042939
Other languages
French (fr)
Other versions
WO2002042261A2 (en
WO2002042261A8 (en
Inventor
Wayne Douglas Luke
Heidi Ann Sanderson
Hua Zheng
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Priority to AU2002228593A priority Critical patent/AU2002228593A1/en
Priority to AU2002228593A priority patent/AU2002228593A8/en
Publication of WO2002042261A2 publication Critical patent/WO2002042261A2/en
Publication of WO2002042261A3 publication Critical patent/WO2002042261A3/en
Anticipated expiration legal-status Critical
Publication of WO2002042261A8 publication Critical patent/WO2002042261A8/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56—Radicals substituted by oxygen atoms

Landscapes

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

Abstract

The present invention relates to a biphasic process for preparing a compound of formula (I) from a compound a compound of formula (II) and (III).
PCT/US2001/042939 2000-11-27 2001-11-14 PROCESS FOR PREPARING α-(3-ARYLTHIO)-ACETOPHENONES Ceased WO2002042261A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2002228593A AU2002228593A1 (en) 2000-11-27 2001-11-14 Process for preparing alpha-(3-arylthio)-acetophenones
AU2002228593A AU2002228593A8 (en) 2000-11-27 2001-11-14 Process for preparing alpha-(3-arylthio)-acetophenones

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25307300P 2000-11-27 2000-11-27
US60/253,073 2000-11-27

Publications (3)

Publication Number Publication Date
WO2002042261A2 WO2002042261A2 (en) 2002-05-30
WO2002042261A3 true WO2002042261A3 (en) 2003-03-06
WO2002042261A8 WO2002042261A8 (en) 2008-04-24

Family

ID=22958714

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/042939 Ceased WO2002042261A2 (en) 2000-11-27 2001-11-14 PROCESS FOR PREPARING α-(3-ARYLTHIO)-ACETOPHENONES

Country Status (2)

Country Link
AU (2) AU2002228593A8 (en)
WO (1) WO2002042261A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002042289A2 (en) 2000-11-27 2002-05-30 Eli Lilly And Company Process for preparing 3-aryl-benzo[b]thiophenes
EP1546138B1 (en) 2002-09-30 2012-01-18 A/S GEA Farmaceutisk Fabrik Raloxifene l-lactate or a hemihydrate thereof, their uses, pharmaceutical compositions and preparation processes
DE10309645A1 (en) * 2003-03-06 2004-09-16 Basf Ag Process for the preparation of a- (3-arylthio) acetophenones

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
A.D. PALKOWITZ, ET AL.: "Discovery and synthesis of [6-hydroxy-3-[4-[2-(1- piperdinyl)-ethoxy]phenoxy]-2-(4- hydroxyphenyl)]benzo[b]thiophene: a novel, highly potent, selective oestrogen receptor modulator", JOURNAL OF MEDICINAL CHEMISTRY, vol. 40, no. 10, 9 May 1997 (1997-05-09), American Chemical Society, Washington, DC, US, pages 1407 - 1416, XP002217620, ISSN: 0022-2623 *
C.D. JONES, ET AL.: "Antioestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4- hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1- piperidinyl)ethoxy]phenyl]methanone hydrochloride (LY156758), a remarkably effective oestrogen anganonist", JOURNAL OF MEDICINAL CHEMISTRY, vol. 27, no. 8, August 1984 (1984-08-01), American Chemical Society, Washington, DC, US, pages 1057 - 1066, XP000560343, ISSN: 0022-2623 *
S. KIM, ET AL.: "A facile synthesis of 3-aryl-substituted-benzothiophenes via a Lewis acid mediated cyclisation of 2-arylthio-acetophenones", TETRAHEDRON LETTERS, vol. 40, no. 15, 1999, Elsevier Science Publishers, Amsterdam, NL, pages 2909 - 2912, XP001068955, ISSN: 0040-4039 *

Also Published As

Publication number Publication date
WO2002042261A2 (en) 2002-05-30
AU2002228593A1 (en) 2002-06-03
WO2002042261A8 (en) 2008-04-24
AU2002228593A8 (en) 2008-06-12

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