New Synthetic Methods for Benzyloxycarbonyl-l-arginine-p-nitroanilide, Benzoyl-l-arginine-p-nitroanilide, and Acetyl-l-arginine-p-nitroanilide

Abstract
The optically active substrates for two peptidases, benzoyl-l-arginine-p-nitroanilide hydrochloride (l-BAPA·HCl) and acetyl-l-arginine-p-nitroanilide (l-AAPA·HCl), were readily prepared through the synthesis of benzyloxycarbonyl-l-arginine-p-nitroanilide hydrochloride (l-ZAPA·HCl). Benzyloxycarbonyl-l-arginine and p-nitroaniline were directly coupled without any racemization. The product, l-ZAPA·HCl, was quantitatively debenzyloxycarbonylated with hydrogen chloride in glacial acetic acid at 50 °C to l-arginine-p-nitroanilide dihydrochloride(l-APA·2HCl) which gave, on benzoylation or acetylation, l-BAPA·HCl or l-AAPA·HCl respectively.

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