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WO1999065318A3 - Germinal substituierte amine - Google Patents

Germinal substituierte amine Download PDF

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Publication number
WO1999065318A3
WO1999065318A3 PCT/EP1999/004256 EP9904256W WO9965318A3 WO 1999065318 A3 WO1999065318 A3 WO 1999065318A3 EP 9904256 W EP9904256 W EP 9904256W WO 9965318 A3 WO9965318 A3 WO 9965318A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
cycloalkyl
substituted amines
alkinyl
cycloalkenyl
Prior art date
Application number
PCT/EP1999/004256
Other languages
English (en)
French (fr)
Other versions
WO1999065318A2 (de
Inventor
Herwig Buchholz
Urs Welz-Biermann
Original Assignee
Merck Patent Gmbh
Herwig Buchholz
Urs Welz-Biermann
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
Priority claimed from DE19827161A external-priority patent/DE19827161A1/de
Priority claimed from DE19827163A external-priority patent/DE19827163A1/de
Priority claimed from DE19827166A external-priority patent/DE19827166A1/de
Priority claimed from DE19827165A external-priority patent/DE19827165A1/de
Priority claimed from DE19827164A external-priority patent/DE19827164A1/de
Priority claimed from DE19844194A external-priority patent/DE19844194A1/de
Application filed by Merck Patent Gmbh, Herwig Buchholz, Urs Welz-Biermann filed Critical Merck Patent Gmbh
Priority to EP99932703A priority Critical patent/EP1088029A1/de
Priority to JP2000554208A priority patent/JP2003524588A/ja
Priority to KR1020007014315A priority patent/KR20010072617A/ko
Publication of WO1999065318A2 publication Critical patent/WO1999065318A2/de
Publication of WO1999065318A3 publication Critical patent/WO1999065318A3/de

Links

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
    • C07D295/02—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/023—Preparation; Separation; Stabilisation; Use of additives
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/0201—Oxygen-containing compounds
    • B01J31/0211—Oxygen-containing compounds with a metal-oxygen link
    • B01J31/0212—Alkoxylates
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/0234—Nitrogen-, phosphorus-, arsenic- or antimony-containing compounds
    • B01J31/0235—Nitrogen containing compounds
    • B01J31/0237—Amines
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/0272—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing elements other than those covered by B01J31/0201 - B01J31/0255
    • B01J31/0274—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing elements other than those covered by B01J31/0201 - B01J31/0255 containing silicon
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/66—Preparation of compounds containing amino groups bound to a carbon skeleton from or via metallo-organic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • 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
    • C07D295/02—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03—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 containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2231/00—Catalytic reactions performed with catalysts classified in B01J31/00
    • B01J2231/40—Substitution reactions at carbon centres, e.g. C-C or C-X, i.e. carbon-hetero atom, cross-coupling, C-H activation or ring-opening reactions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

Amin der allgemeinen Formel (I): wobei R?1 und R2¿ gleich oder verschieden sein können und jeweils einzeln unabhängig voneinander für substituiertes oder unsubstituiertes Alkyl, Cycloalkyl, Alkenyl, Cycloalkenyl, Alkinyl, Aryl oder Trialkylsilyl stehen oder R?1 und R2¿ zusammen mit dem Stickstoffatom an das sie gebunden sind einen substituierten oder unsubstituierten Cycloalkylring bilden können, der neben dem Stickstoffatom noch mindestens ein weiteres Heteroatom enthalten kann, das ausgewählt ist aus der Gruppe bestehend aus Stickstoff, Sauerstoff oder Schwefel, R3 ausgewählt ist aus Wasserstoff und Methyl, das gegebenfalls mit 1-3 Fluoratomen substituiert sein kann, R?4 und R5¿ gleich oder verschieden sein können und jeweils einzeln unabhängig voneinander für substituiertes oder unsubstituiertes Alkyl, Cycloalkyl, Alkenyl, Cycloalkenyl, oder Alkinyl stehen; oder ein Salz davon.
PCT/EP1999/004256 1998-06-18 1999-06-18 Germinal substituierte amine WO1999065318A2 (de)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP99932703A EP1088029A1 (de) 1998-06-18 1999-06-18 Germinal substituierte amine
JP2000554208A JP2003524588A (ja) 1998-06-18 1999-06-18 ジェミナルに置換されたアミン
KR1020007014315A KR20010072617A (ko) 1998-06-18 1999-06-18 동일 자리 탄소가 치환된 아민

Applications Claiming Priority (14)

Application Number Priority Date Filing Date Title
DE19827161A DE19827161A1 (de) 1998-06-18 1998-06-18 Verfahren zur katalytischen, symmetrischen Disubstitution von Carbonsäureamiden mit Grignardreagenzien
DE19827163A DE19827163A1 (de) 1998-06-18 1998-06-18 Verfahren zur katalytischen, unsymmetrischen Disubstitution von Carbonsäureamiden mit 2 unterschiedlichen Grignardreagenzien
DE19827161.1 1998-06-18
DE19827166.2 1998-06-18
DE19827166A DE19827166A1 (de) 1998-06-18 1998-06-18 Verfahren zur katalytischen Disubstitution von Carbonsäureamiden mit wenigstens einem Grignardreagenz
DE19827165A DE19827165A1 (de) 1998-06-18 1998-06-18 Katalytisch Titan(IV)-oxid-vermittelte geminale unsymmetrische Dialkylierung von Carbonsäureamiden
DE19827164.6 1998-06-18
DE19827165.4 1998-06-18
DE19827167 1998-06-18
DE19827167.0 1998-06-18
DE19827164A DE19827164A1 (de) 1998-06-18 1998-06-18 Katalytisch Titan(IV)-oxid vermittelte geminale symmetrische Dialkylierung von Carbonsäureamiden
DE19827163.8 1998-06-18
DE19844194.0 1998-09-26
DE19844194A DE19844194A1 (de) 1998-06-18 1998-09-26 Verfahren zur symmetrischen oder unsymmetrischen Disubstitution von Carbonsäureamiden mit Organotitanaten und Grignardreagenzien

Publications (2)

Publication Number Publication Date
WO1999065318A2 WO1999065318A2 (de) 1999-12-23
WO1999065318A3 true WO1999065318A3 (de) 2003-04-17

Family

ID=27561759

Family Applications (4)

Application Number Title Priority Date Filing Date
PCT/EP1999/004258 WO1999065864A2 (de) 1998-06-18 1999-06-18 Geminal substituierte amine
PCT/EP1999/004256 WO1999065318A2 (de) 1998-06-18 1999-06-18 Germinal substituierte amine
PCT/EP1999/004255 WO1999065855A2 (de) 1998-06-18 1999-06-18 Kombinatorische bibliotheken geminal substituierter amine
PCT/EP1999/004257 WO1999065863A1 (de) 1998-06-18 1999-06-18 Verfahren zur herstellung von kombinatorischen aminbibliotheken

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/EP1999/004258 WO1999065864A2 (de) 1998-06-18 1999-06-18 Geminal substituierte amine

Family Applications After (2)

Application Number Title Priority Date Filing Date
PCT/EP1999/004255 WO1999065855A2 (de) 1998-06-18 1999-06-18 Kombinatorische bibliotheken geminal substituierter amine
PCT/EP1999/004257 WO1999065863A1 (de) 1998-06-18 1999-06-18 Verfahren zur herstellung von kombinatorischen aminbibliotheken

Country Status (3)

Country Link
EP (2) EP1087929A1 (de)
JP (2) JP2002518366A (de)
WO (4) WO1999065864A2 (de)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19960377A1 (de) * 1999-12-14 2001-06-21 Merck Patent Gmbh Verfahren zur Herstellung kombinatorischer Aminbibliotheken
DE19961372A1 (de) * 1999-12-17 2001-06-21 Merck Patent Gmbh Verfahren zur Herstellung kombinatorischer Bibliotheken arylsubstituierter Amine
KR101878361B1 (ko) * 2010-09-20 2018-08-20 시르나 쎄러퓨틱스 인코퍼레이티드 올리고뉴클레오티드 전달을 위한 신규 저분자량 양이온성 지질
GB201208775D0 (en) * 2012-05-18 2012-07-04 Uni I Oslo Chemical compounds

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB807835A (en) * 1955-07-01 1959-01-21 Thomae Gmbh Dr K New tertiary amines and their salts and process for their preparation
GB921943A (en) * 1959-11-25 1963-03-27 Lilly Co Eli Anti-hypertensive compositions
US4020059A (en) * 1975-06-02 1977-04-26 Nippon Shokubai Kagaku Kogyo Co., Ltd. Process for preparing tertiary amines
DE2725245A1 (de) * 1976-06-03 1977-12-15 Labaz Methylaminderivate, verfahren zu deren herstellung und diese enthaltende pharmazeutische oder veterinaermedizinische zusammensetzungen
DE2657476A1 (de) * 1976-12-18 1978-06-22 Basf Ag Morpholinderivate
WO1998000398A1 (en) * 1996-06-28 1998-01-08 University Of Southern California Method for the synthesis of amines and amino acids with organoboron derivatives

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2207137A1 (en) * 1996-06-14 1997-12-14 James Erwin Fritz Scavenger assisted combinatorial process for preparing libraries of secondary amine compounds

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB807835A (en) * 1955-07-01 1959-01-21 Thomae Gmbh Dr K New tertiary amines and their salts and process for their preparation
GB921943A (en) * 1959-11-25 1963-03-27 Lilly Co Eli Anti-hypertensive compositions
US4020059A (en) * 1975-06-02 1977-04-26 Nippon Shokubai Kagaku Kogyo Co., Ltd. Process for preparing tertiary amines
DE2725245A1 (de) * 1976-06-03 1977-12-15 Labaz Methylaminderivate, verfahren zu deren herstellung und diese enthaltende pharmazeutische oder veterinaermedizinische zusammensetzungen
DE2657476A1 (de) * 1976-12-18 1978-06-22 Basf Ag Morpholinderivate
WO1998000398A1 (en) * 1996-06-28 1998-01-08 University Of Southern California Method for the synthesis of amines and amino acids with organoboron derivatives

Non-Patent Citations (15)

* Cited by examiner, † Cited by third party
Title
"BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE, vierte Auflage, drittes Ergänzungswerk, Band IV, erster Teil, S. 308, 428", 1962, SPRINGER-VERLAG, BERLIN . GÖTTINGEN . HEIDELBERG, XP002118210 *
"BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE, vierte Auflage, drittes Ergänzungswerk, Band XII, vierter Teil, S. 2223-2224", 1972, SPRINGER-VERLAG, BERLIN . HEIDELBERG . NEW YORK, XP002118212 *
"BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE, vierte Auflage, drittes und viertes Ergänzungswerk, Bd 20, erster Teil, S. 316", 1977, SPRINGER-VERLAG, BERLIN . HEIDELBERG . NEW YORK, XP002117681 *
"BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE, vierte Auflage, viertes Ergänzungswerk, Band IV, erster Teil, S. 689, 745", 1977, SPRINGER-VERLAG, BERLIN . HEIDELBERG . NEW YORK, XP002118211 *
"BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE, vierte Auflage, viertes Ergänzungswerk, Band XII, vierter Teil, S. 2182", 1984, SPRINGER-VERLAG, BERLIN . HEIDELBERG . NEW YORK . TOKYO, XP002118213 *
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KUFFNER F. ET AL.: "Über hochverzweigte aliphatische Verbindungen", MONATSHEFTE FÜR CHEMIE, vol. 93, 1962, pages 499 - 475, XP002117676 *
MICHAEL B. SMITH ET AL.: "Reaction of amines with cyclopropylcarbinyl halides", JOURNAL OF ORGANIC CHEMISTRY., vol. 50, no. 24, 1985, EASTON US, pages 4815 - 4821, XP002118209 *
N. MAXIM ET AL.: "Sur la méthode de Bouveault ....", BULLETIN DE LA SOCIETE CHIMIQUE DE FRANCE., vol. 5, no. 3, 1936, SOCIETE FRANCAISE DE CHIMIE. PARIS., FR, pages 1084 - 1093, XP002117677, ISSN: 0037-8968 *
R. LUKÈS ET AL.: "Die Spaltung verzweigter, optisch aktiver tertiärer basen", COLLECTION CZECHOSLOVAK CHEMICAL COMMUNICATIONS, vol. 24, 1959, pages 110 - 115, XP002117675 *
R. LUKÈS ET AL.: "Über die Spaltung verzweigter tertiärer Basen II.", COLLECTION CZECHOSLOVAK CHEMICAL COMMUNICATIONS, vol. 25, 1960, pages 461 - 464, XP002117678 *

Also Published As

Publication number Publication date
JP2002518366A (ja) 2002-06-25
WO1999065318A2 (de) 1999-12-23
WO1999065855A2 (de) 1999-12-23
JP2003524588A (ja) 2003-08-19
WO1999065864A2 (de) 1999-12-23
WO1999065864A3 (de) 2003-05-22
EP1087929A1 (de) 2001-04-04
WO1999065855A3 (de) 2003-12-11
WO1999065863A1 (de) 1999-12-23
EP1088029A1 (de) 2001-04-04

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