Epoxides are important heterocyclic units found in various naturally occurring molecules, some with potential bioactivities. At least fourteen drugs on the market are epoxide-containing. In addition, epoxides are valuable building blocks in medicinal chemistry. They react with nucleophiles in a ring-opening process to form new C-C, C-O and C-N bonds. Herein we have designed and synthesized a library of small heteroaliphatic epoxides for drug design.
Design
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>100 unique epoxides on a 5-50 g scale from stock.
More than 100 FDA-approved drugs contain pyridine ring and another 100 have been in clinical trials. Examples containing CF3-pyridine moiety include the antiviral drug Tipranavir and drug candidates Taranabant, Velneperit, SB-705498. Besides, CF3-pyridine containing compounds have been playing a fundamental role in agrochemistry. The introduction of fluorine-containing group alters important pharmacokinetic properties of molecular scaffolds. Herein we have designed and synthesized a library of CF3-substituted pyridine analogues for drug design and agrochemistry.
Design
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>100 unique CF3-pyridine analogues on a 5-50 g scale from stock
More than 100 FDA-approved drugs contain the piperazine moiety. Piperazine-based analogues may advantageously alter important pharmacokinetic properties when grafted onto molecular scaffolds. In 2018, chemists showed that replacing a piperazine ring in the drug Olaparib with the spirodiamine analogue beneficially affected activity and reduced cytotoxicity of the parent compound. Herein we have designed and synthesized a library of piperazine analogues for drug design.
Design
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>100 unique piperazine analogues on a 5-50 g scale from stock.
Saturated azaheterocycles are popular in modern drug discovery programs. More than 50 FDA-approved drugs containing a fragment of pyrrolidine and piperidine have appeared on the market. Pyrrolidine/piperidine-based azasugars and their analogues are potent glycosidase inhibitors. These unique molecules promise a new generation of iminosugar-based medicines for a wide range of diseases. For example, a bioactive azasugar includes the anti-diabetic drug Glyset. In this context, herein we have designed and synthesized a library of sugar-like derivatives for drug design.
Design
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>50 unique sugar-like derivatives on a 5-50 g scale in stock.
Organic azides are an important class of synthetic building blocks commonly used for “Click Chemistry” via Cu(I)-catalyzed Huisgen azide-alkyne 1,3-dipolar cycloaddition reaction.
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Our stock of azides contains over 1 100 building blocks having various residues:
We have developed the library of 380 diverse azides that can be used for click chemistry. The building blocks are supplied in DMSO solutions at 100 mM. Most popular library formats available for immediate supply are shown below. You can suggest your preferred format and also select your own set of azides.
Most popular library formats available for immediate supply
Catalog No.
AZD-380-X-100
Compounds
380
Plates
4
Amount
100 µL of 100 mM DMSO stock solutions
Format
96-well microplates, 96 compounds per plate
Our azide libraries have balanced profiles representing various types of azides ranging from aliphatic to heteroaromatic ones. These building blocks have been approved for parallel synthesis after tests conducted at Enamine. Many azides are rare and not available at the market, besides at Enamine. All building blocks can be resupplied in larger amounts in e.g. MTBE solutions allowing transportation by air.
380 Diverse Azides Profile
MW distribution for 380 Diverse Azides
Understanding the importance of the fast access to the diverse building blocks used in Click Chemistry, Enamine offers several collections of compounds providing access to many classes of organic fragments – heterocyclic rings, aromatic, heteroaromatic, aliphatic residues, functionalized by different functional groups.
Acetylenes for "Click Chemistry"
Molecular properties
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Enamine offers world class service in chemical synthesis of a wide variety of organic compounds on the milligram to kilogram scale at competitive price.