Building Blocks

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<p>Versatile small molecule scaffold</p>

<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>Naphthalene-2-carboximidamide is a benzamidine derivative that interacts with the active site of serine proteases. It was shown to have potent inhibitory potency against a number of proteinases, including urokinase-type plasminogen activator (uPA), matrix metalloproteinase-9 (MMP-9), and cathepsin G. The interaction of naphthalene-2-carboximidamide with uPA was specific and led to inhibition of its catalytic activity. Naphthalene-2-carboximidamide has been tested in clinical trials for the treatment of influenza.</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>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>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>Versatile small molecule scaffold</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>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>