WO2001044160A3 - Verfahren zur herstellung kombinatorischer aminbibliotheken - Google Patents

Verfahren zur herstellung kombinatorischer aminbibliotheken Download PDF

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Publication number
WO2001044160A3
WO2001044160A3 PCT/EP2000/012172 EP0012172W WO0144160A3 WO 2001044160 A3 WO2001044160 A3 WO 2001044160A3 EP 0012172 W EP0012172 W EP 0012172W WO 0144160 A3 WO0144160 A3 WO 0144160A3
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substituted
different
cycloalkyl
cycloalkenyl
alkynyl
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PCT/EP2000/012172
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English (en)
French (fr)
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WO2001044160A2 (de
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Herwig Buchholz
Urs Welz-Biermann
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Merck Patent Gmbh
Herwig Buchholz
Welz Biermann Urs
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Priority to AU23623/01A priority Critical patent/AU2362301A/en
Publication of WO2001044160A2 publication Critical patent/WO2001044160A2/de
Publication of WO2001044160A3 publication Critical patent/WO2001044160A3/de

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    • 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
    • B01J31/0214—Aryloxylates, e.g. phenolates
    • 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
    • B01J31/0272—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
    • 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
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/03—Monoamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/03—Monoamines
    • C07C211/08—Monoamines containing alkyl groups having a different number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/16—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings other than six-membered aromatic rings
    • C07C211/17—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of a saturated carbon skeleton containing rings other than six-membered aromatic rings containing only non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/20—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton
    • C07C211/21—Monoamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/35—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing only non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C211/44—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
    • C07C211/45—Monoamines
    • C07C211/48—N-alkylated amines
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • 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
    • B01J21/00—Catalysts comprising the elements, oxides, or hydroxides of magnesium, boron, aluminium, carbon, silicon, titanium, zirconium, or hafnium
    • B01J21/06—Silicon, titanium, zirconium or hafnium; Oxides or hydroxides thereof
    • 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
    • B01J21/00—Catalysts comprising the elements, oxides, or hydroxides of magnesium, boron, aluminium, carbon, silicon, titanium, zirconium, or hafnium
    • B01J21/06—Silicon, titanium, zirconium or hafnium; Oxides or hydroxides thereof
    • B01J21/063—Titanium; Oxides or hydroxides thereof
    • 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
    • B01J21/00—Catalysts comprising the elements, oxides, or hydroxides of magnesium, boron, aluminium, carbon, silicon, titanium, zirconium, or hafnium
    • B01J21/10—Magnesium; Oxides or hydroxides thereof
    • 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
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • 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
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Die vorliegende Erfindung betrifft eine kombinatorische Bibliothek umfassend mindestens zwei verschiedene Amine der allgemeinen Formeln (I) und/oder (Ia), worin 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. Gegenstand der Erfindung ist ebenfalls ein Verfahren zur Herstellung von kombinatorischen Bibliotheken, umfassend mindestens Amine der allgemeinen Formeln.
PCT/EP2000/012172 1999-12-14 2000-12-04 Verfahren zur herstellung kombinatorischer aminbibliotheken WO2001044160A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU23623/01A AU2362301A (en) 1999-12-14 2000-12-04 Method for producing combinatorial amine libraries

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DE19960377.4 1999-12-14
DE19960377A DE19960377A1 (de) 1999-12-14 1999-12-14 Verfahren zur Herstellung kombinatorischer Aminbibliotheken

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WO2001044160A3 true WO2001044160A3 (de) 2002-03-07

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Families Citing this family (1)

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EP3144015B1 (de) * 2010-09-20 2021-06-02 Sirna Therapeutics, Inc. Kationische lipide mit geringem molekulargewicht zur oligonukleotidabgabe

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* 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
EP0029617A1 (de) * 1979-11-27 1981-06-03 C.F. Spiess & Sohn GmbH & Co. Chemische Fabrik Verwendung tertiärer heterocyclischer Amine als Potenzierungsmittel für Insektizide; Cyclo-Amin-Derivate
WO1998000398A1 (en) * 1996-06-28 1998-01-08 University Of Southern California Method for the synthesis of amines and amino acids with organoboron derivatives
EP0818431A1 (de) * 1996-06-14 1998-01-14 Eli Lilly And Company Kombinatorisches Verfahren unter Verwendung von Fängerverbindungen zur Herstellung von Bibliotheken von sekundären Aminverdindungen
WO1999065857A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Katalytisch titan(iv)-oxid vermittelte geminale unsymmetrische dialkylierung von carbonsäureamiden
WO1999065864A2 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Geminal substituierte amine
WO1999065861A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Verfahren zur symmetrischen und unsymmetrischen disubstitution von carbonsäureamiden mit organotitanaten und grignard-reagenzien
WO1999065859A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Katalytisch titan(iv)-oxid vermittelte geminale symmetrische dialkylierung von carbonsäureamiden
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EP0029617A1 (de) * 1979-11-27 1981-06-03 C.F. Spiess & Sohn GmbH & Co. Chemische Fabrik Verwendung tertiärer heterocyclischer Amine als Potenzierungsmittel für Insektizide; Cyclo-Amin-Derivate
EP0818431A1 (de) * 1996-06-14 1998-01-14 Eli Lilly And Company Kombinatorisches Verfahren unter Verwendung von Fängerverbindungen zur Herstellung von Bibliotheken von sekundären Aminverdindungen
WO1998000398A1 (en) * 1996-06-28 1998-01-08 University Of Southern California Method for the synthesis of amines and amino acids with organoboron derivatives
WO1999065857A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Katalytisch titan(iv)-oxid vermittelte geminale unsymmetrische dialkylierung von carbonsäureamiden
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WO1999065861A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Verfahren zur symmetrischen und unsymmetrischen disubstitution von carbonsäureamiden mit organotitanaten und grignard-reagenzien
WO1999065859A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Katalytisch titan(iv)-oxid vermittelte geminale symmetrische dialkylierung von carbonsäureamiden
WO1999065860A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Verfahren zur katalytischen disubstitution von carbonsäureamiden mit wenigstens einem grignard-reagenz
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AU2362301A (en) 2001-06-25
WO2001044160A2 (de) 2001-06-21

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