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Solid support

A solid support, support technology, used in biochemical equipment and methods, microbial determination/inspection, instruments, etc.

Active Publication Date: 2020-12-22
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Therefore, there is currently no general and practical method for reacting DNA-binding molecules in anhydrous organic solvents for the purpose of DNA-encoded library synthesis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0293] Example preparation

[0294] The following examples have been prepared, isolated and characterized using the methods disclosed herein.

[0295] abbreviation

[0296] Abbreviations as used herein are defined as follows: "1x" means once, "2x" means twice, "3x" means three times, "°C" means degrees Celsius, "aq" means aqueous, "Col" means column, "eq" means equivalent (equivalent or equivalents), "g" means gram (gram or grams), "mg" means milligram (milligram or milligrams), "nm" means nanometer (nanometer or nanometers), "L" means liter (liter or liters), "mL" or "ml" means milliliter or milliliters, "ul", "uL", "μl", or "μL" means microliter (microliter or microliters), "nL" or "nl" means nanoliter (nanoliter or nanoliters), "N" means normal, "uM" or "μM" means micromole, "nM" means nanomole, "mol" means mole (mole or moles), "mmol" means millimole (millimole or millimoles), "min" means minutes (minute or minutes), "h" or "hrs" means hours (hour or hours), "RT" means ...

example 1

[0350] Synthesis of Cationic Acid 10-Carboxyl-N,N,N-Trimethyldecane 1-Ammonium Bromide

[0351]

[0352] 11-Bromoundecanoic acid (Fluka CAS 2834-05-1) (8 g, 30.2 mmol) was dissolved in trimethylamine (35% in EtOH) (60 ml, 224 mmol), and the reaction vessel was sealed with a septum, at room temperature The solution was stirred for 48 hours. A white precipitate formed at this stage. The white precipitate was filtered and washed with cold EtOH. The collected white solid was recrystallized from EtOH, filtered and dried under reduced pressure to give pure 10-carboxy-N,N,N-trimethyldecane-1-ammonium bromide as a white powder.

[0353] 1 H NMR (400MHz, DMSO-d6) δ3.30-3.24 (m, 2H), 3.04 (s, 9H), 2.19 (t, J = 7.3Hz, 2H), 1.71-1.60 (m, 2H), 1.48 ( t, J=7.1 Hz, 2H), 1.27 (d, J=11.5 Hz, 12H).

[0354] UPLC-MS: 0.51 min; 244.3 (M)+. (2_MIN_REACTION_MONITORING_IPA): Waters UPLC Acquity; Column: Acquity UPLC BEH C18, 1.7μm, 2.1x50mm, at 80°C, Eluent A: H 2 O+0.05% HCOOH+3.75 mM amm...

example 2

[0356] Commercially available NovaPEG resin Rink amide was obtained. The resin NovaPEG resin Rink amide (250 mg) (0.250 g, 0.115 mmol) was swelled in DMF for 3 hours.

[0357] Convert the resin by adding the cationic acid:

[0358] (0.460 mmol), HOAt (0.063 g, 0.460 mmol), and DIC (0.072 mL, 0.460 mmol) were mixed in DMF (volume: 5 mL) / DMSO (volume: 3 mL). The resulting solution was added to the resin and allowed to react for 2 hours. This process was repeated once using only DMSO as solvent. The Kaiser test for free amines was negative.

[0359] Resulting Derivatized Resin:

[0360]

[0361] Wash four times with DMSO and four times with water.

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Abstract

A solid support for use in non-aqueous DNA-conjugated molecule reactions, wherein the support comprises a solid body formed from a plurality of polyethylene glycol units, wherein the solid body includes at least one cationic moiety.

Description

technical field [0001] The present invention relates to solid supports suitable for use in non-aqueous chemical reactions, for example in chemical reactions on or in the presence of DNA to synthesize DNA-encoded libraries (DELs), and also to methods of using these solid supports , the method comprising the steps of adsorbing DNA onto a solid support of the invention and reacting a DNA-labeled compound with a reagent in a non-aqueous solvent system. Background technique [0002] A DNA-encoded library (DEL) is a collection of thousands to billions of synthetic small molecules, each conjugated to a unique DNA sequence used as a structural identifier. These vast collections of synthetic small molecule-DNA conjugates can be screened in a mixture through an affinity selection process, making them attractive tools for the discovery of ligands to pharmaceutical biomolecular targets of interest. Reactions for the synthesis of DELs typically involve the formation of covalent chemical...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C237/06C07K5/00C40B50/14C07K5/11C07C237/04C07C237/08C07C237/12C12Q1/00
CPCC07B2200/11C07C237/06C07K5/1019C40B50/14C07C237/04C07C237/12C07C237/08C07C2601/14G01N33/545C40B20/04
Inventor F·贝尔斯特Y·鲁夫
Owner NOVARTIS AG
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