Building Blocks

<p>2,​3-​Dihydro-3-​thiopheneacetic acid 1,​1-​dioxide is a nucleophilic reagent that can be used to synthesize amides. It reacts with amines to form 2,​3-​dihydro-3-​thiophenecarboxylic acid 1,​1-diamide. Reactions of this compound with heterocycles such as pyridine and quinoline result in the formation of heterocyclic amines.</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>3-(Hydroxymethyl)cyclobutan-1-one is a synthetic piperazine derivative that has been shown to have antitumor and antimycobacterial activities. It is a selective inhibitor of the enzyme purine nucleoside phosphorylase (PNP), which catalyzes the conversion of inosine monophosphate (IMP) to xanthosine monophosphate (XMP). This inhibition results in an accumulation of IMP and deoxyinosine monophosphate (dIMP) in tumor cells. 3-(Hydroxymethyl)cyclobutan-1-one also inhibits Mycobacterium tuberculosis, but not other bacteria such as Escherichia coli or Staphylococcus aureus. The product is synthetically produced by reacting cyclobutanone with hydroxylamine.</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>PB-22 is a synthetic cannabinoid, which can be classified as a CB1 receptor agonist. It is one of the many cannabinoids that have been created in an attempt to circumvent drug laws by creating compounds that are similar to those found in cannabis but have different chemical structures. PB-22 has shown to increase locomotor activity and stimulate the cb1 receptor in mice. Magnetic resonance spectroscopy (MRS) and assays were used to determine the binding affinity of PB-22 for the CB1 receptor. The MRS data showed that PB-22 bound with high affinity to the CB1 receptor and had a lower affinity for CB2 receptors. This suggests that PB-22 may be more potent than other synthetic cannabinoids, such as JWH-018 and CP 55,940, which bind better with CB2 receptors than CB1 receptors.<br>PB-22 is an analog of JWH-073 and has been shown to have a stronger effect on locomotor activity than JWH</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>2-Ethynyl-4-methylthiazole is a cell-based kinase inhibitor that binds to the ATP binding site on the enzyme and inhibits phosphorylation. It was shown to inhibit cell growth in vitro by interfering with the production of TGF-β, activin, and other growth factors. The inhibitory activity of 2-Ethynyl-4-methylthiazole is selective for receptor kinases and is not effective against alk5 kinase. This drug has been shown to be an inhibitor of cellular growth in vitro and may be useful for the treatment of cancer.</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>2-Cyano-5-fluorophenol is an organic compound that is used as a precursor to medicines and other chemicals. It reacts with calcium hydroxide in water to form 2-cyano-5-hydroxyfluorobenzene, which can be hydrolyzed to form 2-cyano-5-chlorofluorobenzene. This compound can also react with sodium hydroxide to produce sodium cyanate, which can be hydrolyzed to form sodium chloride and hydrogen cyanide gas. The alkali metal ions are needed for this reaction, which is why the product should not be exposed to water or moisture. 2-Cyano-5-fluorophenol has been shown to have liquid crystal properties and is used in the production of certain types of polymers. 2Cyano-5Fluorophenol crystals are also used in some medicines such as acetaminophen (paracetamol).</p>

<p>2-Bromo-3,3,3-trifluoro-1-propene is a chemical compound that has been synthesized in an asymmetric reaction. The reactant is bromopropane and the product is 2,2,2-trifluoropropene. The methylene group on the propene molecule is activated by the nucleophilic attack of a fluoride ion from hydrogen fluoride to form a cavity with a highly strained bond. The kinetic study of this reaction revealed that the activation energy for the reaction is 42 kJ/mol. Palladium-catalyzed coupling reactions are catalyzed by palladium and require nonpolar solvents such as toluene or dichloromethane. This type of reaction has been shown to be exothermic with an isolated yield of 1%.</p>

<p>Versatile small molecule scaffold</p>

<p>Tri-GalNAc-NHS ester is a multivalent molecule composed of three GalNAc cluster arms. It is a protein degrader and a ligand of the asialoglycoprotein receptor (ASGPR) used for the development of targeted therapies for liver diseases. The GalNAc arms enable high-affinity binding to the ASGPR on hepatocyte surfaces. The crucial functional group, N-hydroxysuccinimide (NHS) ester, is known for its ease of conjugation with various biomolecules possessing amine (NH2) groups. This biocompatible reaction strategy allows the design and development of targeted conjugates such as drug-GalNAc conjugates, siRNA delivery vehicles, or probes for ASGPR imaging in the liver.</p>