Complex amino acids with an α-acyloxycarbonyl functionality in the side chain are easily available through epoxide opening by chelated enolates and subsequent oxidation/Passerini reaction. This protocol works with both, aldehyde and ketone intermediates, as long as the ketones are activated by electron-withdrawing groups. In principle Ugi reactions are also possible, allowing the generation of ...

Disease management programs typically focus on a few common chronic conditions for which it is possible to simultaneously improve care and reduce costs, such as asthma and diabetes. Insufficient attention has been paid to the management of upper gastrointestinal (UGI) disorders, including peptic ulcer disease, gastritis, dyspepsia, and gastroesophageal reflux disease (GERD), although there are ...

The Bacillus subtilis bacteriophage PBS2 uracil-DNA glycosylase inhibitor (Ugi) protein was characterized and shown to form a stable complex with Escherichia coli uracil-DNA glycosylase (Ung). As determined by mass spectrometry, the Ugi protein had a molecular weight of 9,474. We confirmed this value by sedimentation equilibrium centrifugation and determined that Ugi exists as a monomeric prote...

Novel diterpenic peptide derivatives were synthesized via the Ugi four-component reaction at ambient temperature. The protocol employed a between formaldehyde, benzyl amine, corresponding diterpene acid, and ethyl 2-isocyanoacetate. anticancer properties of compounds studied in vitro.

Efficient one-pot Ugi-Smiles couplings are reported for the use of furyl-substituted aldehyde components. In the presence of these heterocyclic aldehydes, reactions tolerated variations in amine components and led to either isolated N-arylamide Ugi-Smiles adducts or N-arylepoxyisoindolines, products of tandem Ugi-Smiles Diels-Alder cyclizations, in moderate yields. A thienyl-substituted aldehyd...

BACKGROUND AND STUDY AIMS Upper gastrointestinal (UGI) cancer in the Western world usually presents at an advanced stage, when opportunities for curative therapy are limited. The failure to detect subtle, early-stage UGI cancer at endoscopy may contribute to a poor prognosis. We undertook a meta-analysis of studies of endoscopic miss rates for UGI cancer to quantify how often opportunities to d...

The synthesis of multivalent neoglycoconjugates with 2,6-diamino-2,6-dideoxyglucose is accomplished by a flexible Ugi multicomponent approach leading to mono-, di- and tri-valent carbohydrate clusters.

Ammonia and selenoaldehydes are both problematic components in Ugi reactions. Here we report the efficient direct multicomponent synthesis of sensitive selenocysteine peptides without the use of convertible (protected) primary amines, including suitable deprotection protocols for selenols.

The kinetically unstable propargylisocyanide was reacted with the tetrakis(acetonitrile) copper(I) hexafluorophosphate and formed complex then involved in a copper-catalyzed alkyne-azide cycloaddition reaction (CuAAC). After decomplexation of adduct, isocyanide engaged Ugi reaction. By such complexation, reactions can be carried out on CC triple bond without constraint instability free compound...