Benjamin E. Blass

A facile, selective KF/Al2O3 mediated method for the deprotection of aryl silyl ethers and preparation of aryl SEM ethers

Abstract A selective, solvent dependent KF/Al2O3 mediated method for the cleavage of aryl silyl ethers and the preparation of SEM aryl ethers is reported.

Applications of solid supported azide anion: a one-pot, two-step preparation of functionalized 1,2,3-triazoles

Functionalized 1,2,3-triazoles were prepared in a one-pot, two-step synthesis from alkyl halides and alkynes using a polymer supported azide. Two different base resins were examined. The chemistry is suitable for the preparation of combinatorial libraries.

Solid-phase synthesis of functionalized 1,2,3-triazoles

Functionalized 1,2,3-triazoles are prepared by 2+3 cycloaddition of resin bound α-azido esters with substituted alkynes. The reaction is regioselective when the electron-deficient alkyne methyl propiolate is used.

Selective Kv1.5 Blockers: Development of (R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl)-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a Potential Treatment for Atrial Arrhythmia

Atrial fibrillation is the most prevalent form of cardiac arrhythmia. Current treatments extend the atrial effective refractory period by nonselective blockade of cardiac ion channels. An alternative approach selectively targeting the Kv1.5 ion channel offers the opportunity for therapeutic benefit with decreased risk of adverse cardiovascular events. KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent.

A new paradigm for alkene epoxidation: Activation of hydrogen peroxide by organophosphorus electrophiles

Abstract Diphenylphosphinic anhydride and certain other organophosphorus electrophiles mediate the high-yield conversion of alkenes to epoxides by hydrogen peroxide in buffered aqueous tetrahydrofuran.

A FACILE KF/AL2O3 MEDIATED METHOD FOR THE SYNTHESIS OF SUBSTITUTED OXAZOLIDINONES

Abstract 2-Substituted oxazolidinones are prepared by a KF/Al 2 O 3 mediated reaction of an oxazolidinone with an alkyl bromide, isocyanate, or sulfonyl chloride.

Solid-phase synthesis of functionalized 1,2,4-triazin-6-ones

The solid supported synthesis of functionalized 1,2,4-triazin-6-ones from resin bound amino acids and acid chlorides is described. A thioamide intermediate is generated with Lawessons reagent, and the final products are cyclized and cleaved from resin with hydrazine. The products are obtained in good yield and purity.

A facile KF/Al2O3 mediated, selective alkylation of benzodiazepin-2,5-diones

Abstract We have developed a new, versatile method for the selective alkylation of benzodiazepin-2,5-diones using KF on Al 2 O 3 . The use of a reagent on a solid support makes this process suitable for the preparation of combinatorial libraries.

Parallel synthesis and evaluation of N-(1-phenylethyl)-5-phenyl-imidazole-2-amines as Na+/K+ ATPase inhibitors

A series of N-(1-phenylethyl)-5-phenyl-imidazole-2-amines was prepared using solution-phase, parallel synthesis and evaluated for Na+/K+ ATPase inhibition.

A simple method for the preparation and selective functionalization of 4,5-diaminopyrazoles

Abstract A simple procedure for the synthesis and further functionalization of 4,5-diaminopyrazoles using mild conditions is reported herein. The desired products were obtained in good yield, and the structures have been confirmed by X-ray crystallography.