N-Monoacylation of Sulfonimidamides
In recent years, N-alkylation, N-acylation and N-arylation of sulfonamides have proven useful in organic and medicinal chemistry for producing bioactive compounds and drug candidates. Sulfonimidamides (SIAs), the aza analogues to sulfonamides, have been introduced as an interesting but underexplored area of chemistry. Functionalization of SIAs has been conducted in medicinal chemistry programs, and recently, Yantao Chen of AstraZeneca Innovative Medicines Cardiovascular and Metabolic Diseases (Mölndal, Sweden) published a convenient synthetic method to produce monoacylated SIA products from TBS-protected starting materials, using a stoichiometric acylating reagent which was prepared by mixing an acyl chloride with one equivalent of pyridazine.
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