Chemical Products – Alex Haahr Gouliaev, Thomas Franch, Michael Anders Godskesen, Kim Birkebaek Jensen, Nuevolution AS

Abstract for “Bifunctional complexes and methods of making and using them”

The present invention relates to a method of synthesizing a bifunctional complex that includes a molecule and an oligonucleotide identifier. The present invention enables a part of the synthesis to be performed in organic solvents. This is when a nascent, bi-functional complex is formed that includes an optionally protected tag and oligonucleotide identification. Another part of the method is preferred to be conducted under conditions that allow for the addition of an Oligonucleotide tag in solution.

Background for “Bifunctional complexes and methods of making and using them”

“Definitions”

“Chemical Definitions”

“Nucleotides”

“Multiple Encoding”

“Starting Situation:”

“Enzymes”

“Chemical Reaction Sites, Reactive Compound Building blocks and Reactive Groups”

“Nucleophilic Substitution by Activation Electrophiles”

“A. Acylating Monomer Blocks (Reactive Compound Building Blocks)”?Principle

“B. Acylation”

“C. Acylation”

“D. Acylation”

“E. Acylation”

“F. Acylation”

“G. Acylation”

“Coumarine and Quinolinon Formation by Heck Reaction followed by a NucleophilicSubstitution”

“H. Acylation”

“Phthalhydrazide Formation through Reaction of Hydrazines & Phthalimides”

“I. Acylation”

“Diketopiperazine formation by reaction of amino acid esters”

“J. Acylation”

“Hydantoin Formation through Reaction of Urea, Cc-Substituted Esters.”

“L. Vinylating Monomer Blocks (Reactive Compound Blocks)”

“M. Heteroatom Electrophiles”

“N. Acylation”

“Benzodiazepinone formation by reaction of Amino Acid Esters & Amino Ketones

“Addition to Carbon Hetero Multiple Bonds”

“O. Wittig/Horner-Wittig-Emmons Reagents”

“Transition Metal Catalysed Reactions.”

“P. Arylation”

“Q. Arylation”

“R. Arylation”

“S. Alkylation”

“T. Alkylation”

“Nucleophilic Substitution by Activation Of Nucleophiles”

“U. Condensations”

“V. Alkylation”

“Cycloadditions”

“W. [2+4] Cycloadditions”

“X. [2+4] Cycloadditions”

“Y. [3+2] Cycloadditions”

“Z. [3+2] Cycloadditions”

“Aromatic nucleophilic substitutions Transition metal catalysed reactions”

“Addition to Carbon Carbon Multiple Bonds”

“Cycloaddition to Multiple Bounds.”

“Addition to Carbon Hetero Multiple Bonds

“Addition of an Alkene to a Primary Amine:

“Nucleophilic Substitution:”

“Reductive Alkylation for an Amine”

“Palladium-Catalyzed Carbon Carbon Bond Forming Reactions”

“Ugi Condensation reactions:

“Electrophilic Aromatic Substitution reactions:

“Cycloaddition Reactions:”

“Diels-Alder Cycloaddition”

“1,3-di[rho]olar Cicloaddition, C?N.O, C.N.S, N3, Nucleophilic Aromtic Substitution Reactions”,

“W is an Electron Withdrawing Group.”

“Heck Reaction:”

“Acetal Formation:”

“Aldol Reactions:”

“A. Acylation Reactions.”

“B. Alkylation”

“C. Vinylation Reactions.”

“D. Alkenylidation reactions”

“E. Transition Metal Catalyzed Hetarylation, Arylation and Vinylation Reactions”

“F. Reactions of Enamine Monomer Reactive Compound Blocks”

“Cross-Link Reactive Compound Block Building Blocks for Cross-Link Cleavage”

“Protection Groups”

“Procedure to tBu Ester or N-Boc Deceprotection”

“Procedure Fmoc Water Deprotection”

“Procedure Msc Water Deprotection”

“Procedure to Fmoc deprotection of DEAE Sepharose”

“Procedure to Ns Deprotection of DEAE Sepharose”

“Procedure to Ns Deprotection of DEAE Sepharose (Parallel format)”

“Scaffolds & Small Molecules”

“Linker Moieties”

“Examples for Linkers Clearable by Electromagnetic Radiation Light”

“Dansyl Derivatives:”

“Coumarin Derivatives”

“DMT=4,4?-Dimethoxytrityl”

“CNEt=Cyanoethyl”

“Examples for Linkers that are Cleavable with Chemical Agents:

“Linkers are cleavable with enzymes”

“Resynthesis of Bifunctional Complexes”

“Templated Synthesis of a Bi-Functional Complex Library Using Identifier Allocation and Sequential Identifier Subtraction.”

“Step 1 – Construction of Complementary Label Columns”

“Step 3 – Chemical Reactions at Point A”

“Chemical Reaction at Point B”

“Chemical Reactions at position C”

“Chemical reactions at position D”

“Library Synthesis Methods.”

“a) Azides”

“b) Diazirines”

“c) Halo-Aromatic/Halo-Heteroaromatic Compounds”

“d) Aromatic Nitro Compounds

“e) Benzophenones”

“f) Enones”

“g” Thiobenzyl Compounds

“Selection Steps & Further Down-Stream Processing steps”

“Tag Amplification”

“i) Providing”

Summary for “Bifunctional complexes and methods of making and using them”

“Definitions”

“Chemical Definitions”

“Nucleotides”

“Multiple Encoding”

“Starting Situation:”

“Enzymes”

“Chemical Reaction Sites, Reactive Compound Building blocks and Reactive Groups”

“Nucleophilic Substitution by Activation Electrophiles”

“A. Acylating Monomer Blocks (Reactive Compound Building Blocks)”?Principle

“B. Acylation”

“C. Acylation”

“D. Acylation”

“E. Acylation”

“F. Acylation”

“G. Acylation”

“Coumarine and Quinolinon Formation by Heck Reaction followed by a NucleophilicSubstitution”

“H. Acylation”

“Phthalhydrazide Formation through Reaction of Hydrazines & Phthalimides”

“I. Acylation”

“Diketopiperazine formation by reaction of amino acid esters”

“J. Acylation”

“Hydantoin Formation through Reaction of Urea, Cc-Substituted Esters.”

“L. Vinylating Monomer Blocks (Reactive Compound Blocks)”

“M. Heteroatom Electrophiles”

“N. Acylation”

“Benzodiazepinone formation by reaction of Amino Acid Esters & Amino Ketones

“Addition to Carbon Hetero Multiple Bonds”

“O. Wittig/Horner-Wittig-Emmons Reagents”

“Transition Metal Catalysed Reactions.”

“P. Arylation”

“Q. Arylation”

“R. Arylation”

“S. Alkylation”

“T. Alkylation”

“Nucleophilic Substitution by Activation Of Nucleophiles”

“U. Condensations”

“V. Alkylation”

“Cycloadditions”

“W. [2+4] Cycloadditions”

“X. [2+4] Cycloadditions”

“Y. [3+2] Cycloadditions”

“Z. [3+2] Cycloadditions”

“Aromatic nucleophilic substitutions Transition metal catalysed reactions”

“Addition to Carbon Carbon Multiple Bonds”

“Cycloaddition to Multiple Bounds.”

“Addition to Carbon Hetero Multiple Bonds

“Addition of an Alkene to a Primary Amine:

“Nucleophilic Substitution:”

“Reductive Alkylation for an Amine”

“Palladium-Catalyzed Carbon Carbon Bond Forming Reactions”

“Ugi Condensation reactions:

“Electrophilic Aromatic Substitution reactions:

“Cycloaddition Reactions:”

“Diels-Alder Cycloaddition”

“1,3-di[rho]olar Cicloaddition, C?N.O, C.N.S, N3, Nucleophilic Aromtic Substitution Reactions”,

“W is an Electron Withdrawing Group.”

“Heck Reaction:”

“Acetal Formation:”

“Aldol Reactions:”

“A. Acylation Reactions.”

“B. Alkylation”

“C. Vinylation Reactions.”

“D. Alkenylidation reactions”

“E. Transition Metal Catalyzed Hetarylation, Arylation and Vinylation Reactions”

“F. Reactions of Enamine Monomer Reactive Compound Blocks”

“Cross-Link Reactive Compound Block Building Blocks for Cross-Link Cleavage”

“Protection Groups”

“Procedure to tBu Ester or N-Boc Deceprotection”

“Procedure Fmoc Water Deprotection”

“Procedure Msc Water Deprotection”

“Procedure to Fmoc deprotection of DEAE Sepharose”

“Procedure to Ns Deprotection of DEAE Sepharose”

“Procedure to Ns Deprotection of DEAE Sepharose (Parallel format)”

“Scaffolds & Small Molecules”

“Linker Moieties”

“Examples for Linkers Clearable by Electromagnetic Radiation Light”

“Dansyl Derivatives:”

“Coumarin Derivatives”

“DMT=4,4?-Dimethoxytrityl”

“CNEt=Cyanoethyl”

“Examples for Linkers that are Cleavable with Chemical Agents:

“Linkers are cleavable with enzymes”

“Resynthesis of Bifunctional Complexes”

“Templated Synthesis of a Bi-Functional Complex Library Using Identifier Allocation and Sequential Identifier Subtraction.”

“Step 1 – Construction of Complementary Label Columns”

“Step 3 – Chemical Reactions at Point A”

“Chemical Reaction at Point B”

“Chemical Reactions at position C”

“Chemical reactions at position D”

“Library Synthesis Methods.”

“a) Azides”

“b) Diazirines”

“c) Halo-Aromatic/Halo-Heteroaromatic Compounds”

“d) Aromatic Nitro Compounds

“e) Benzophenones”

“f) Enones”

“g” Thiobenzyl Compounds

“Selection Steps & Further Down-Stream Processing steps”

“Tag Amplification”

“i) Providing”

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