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Method for synthesizing On-DNA dihydropyrazole compound

A technology for dihydropyrazoles and compounds, applied in the field of coding compound libraries, can solve the problems of no reports, etc., and achieve the effects of simple operation, single product, and environmental friendliness

Pending Publication Date: 2021-06-08
HITGEN INC
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0004] Dihydropyrazole compounds are an important class of pharmaceutical compound skeleton structure, but there is no report on the synthesis of On-DNA dihydropyrazole compounds through On-DNA α,β-unsaturated carbonyl compounds

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  • Method for synthesizing On-DNA dihydropyrazole compound
  • Method for synthesizing On-DNA dihydropyrazole compound
  • Method for synthesizing On-DNA dihydropyrazole compound

Examples

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Embodiment 1

[0054] The synthesis of embodiment 1, On-DNA dihydropyrazole compound

[0055] Step 1. Synthesis of On-DNA α, β-unsaturated carbonyl compounds

[0056]

[0057] Dissolve the On-DNA arylethanone compound (1) in 250 mM, pH=9.4 boric acid buffer solution to prepare a 1 mM concentration solution (20 μL, 20 nmol), and add benzaldehyde (4000 nmol, 200 equivalents, 200mM DMSO), potassium hydroxide (10000nmol, 500 equivalents, 500mM double distilled water), mix well, and react at 30°C for 1 hour.

[0058] After the reaction is completed, carry out ethanol precipitation: add a total volume of 10% 5M sodium chloride solution to the reacted solution, and then continue to add 3 times the total volume of absolute ethanol, shake evenly, and place the reaction in dry ice to freeze After 0.5 hours, centrifuge at 12000rpm for half an hour, discard the supernatant, and dissolve the remaining precipitate with deionized water to obtain a solution of On-DNA α, β-unsaturated carbonyl compound (...

Embodiment 2

[0063] Embodiment 2, the synthesis of On-DNA dihydropyrazole compound

[0064]

[0065] Dissolve 22 kinds of On-DNA α, β-unsaturated carbonyl compounds in 250mM, pH=9.4 boric acid buffer solution respectively to prepare 1mM concentration solution (20μL, 20nmol), add hydrazine hydrate (4000nmol, 200 equivalents) to the solution , 200mM double-distilled water), mix well, and react at 30°C for 1 hour.

[0066] After the reaction is completed, carry out ethanol precipitation: add a total volume of 10% 5M sodium chloride solution to the reacted solution, and then continue to add 3 times the total volume of absolute ethanol, shake evenly, and place the reaction in dry ice to freeze After 0.5 hours, centrifuge at 12,000rpm for half an hour, pour off the supernatant, and dissolve the remaining precipitate with deionized water to obtain a solution of On-DNA product. After quantifying the OD with a microplate reader, send it to LCMS to confirm the reaction conversion Rate.

[0067]...

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Abstract

The invention relates to a method for synthesizing an On-DNA dihydropyrazole compound, an On-DNA alpha. The method is characterized in that beta-unsaturated carbonyl compound and a hydrazine compound are used as raw materials to react to obtain the On-DNA dihydropyrazole compound. The reaction method can be carried out in a mixed water phase of an organic solvent / water phase, is simple to operate, introduces no metal reagents, is environmentally friendly, and is suitable for synthesizing a DNA coding compound library by using a porous plate.

Description

technical field [0001] The invention belongs to the technical field of encoded compound libraries, and in particular relates to a method for synthesizing On-DNA dihydropyrazole compounds in the construction of DNA encoded compound libraries. Background technique [0002] In drug development, especially new drug development, high-throughput screening for biological targets is one of the main means to quickly obtain lead compounds. However, the traditional high-throughput screening based on a single molecule requires a long time, huge investment in equipment, limited number of library compounds (millions), and the construction of a compound library requires decades of accumulation, which limits the efficiency and efficiency of lead compound discovery. possibility. The DNA-encoded compound library technology (WO2005058479, WO2018166532, CN103882532) that has emerged in recent years combines combinatorial chemistry and molecular biology techniques to add a DNA tag to each compo...

Claims

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Application Information

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IPC IPC(8): C07H21/04C07H1/00
CPCC07H21/04C07H1/00
Inventor 李进高森杜甜伍荣峰刘观赛万金桥
Owner HITGEN INC
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