1,1,3,3,-Bis-polymethylene-2-(hetero)aryl-uronium salts - are condensn. agents with improved solubility properties, esp. for use in automated peptide syntheses

Uronium salts (I) are new, where X=N-oxido-pyrid-2-one or pentafluorophenoxy; Y=an anion; Z=-(CH2)n- or -(CH2)2-O-(CH2)2-; n=4-6. Y(-) is pref. Cl-, BF4(-) or PF6(-). USE/ADVANTAGE - Cpds. (I) are condensn. agents for the prodn. of peptides, beta-lactams, amides and esters. They are esp. suitable fo...

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Hauptverfasser: HENKLEIN, PETER., O-1130 BERLIN, DE, EUTHIN, ELKE., O-1170 BERLIN, DE, PIPKORN, RUEDIGER., 6900 HEIDELBERG, DE, BAEHR, RUEDIGER VON, DR., O-1020 BERLIN, DE, BEYERMANN, MICHAEL., O-1140 BERLIN, DE
Format: Patent
Sprache:eng ; ger
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Zusammenfassung:Uronium salts (I) are new, where X=N-oxido-pyrid-2-one or pentafluorophenoxy; Y=an anion; Z=-(CH2)n- or -(CH2)2-O-(CH2)2-; n=4-6. Y(-) is pref. Cl-, BF4(-) or PF6(-). USE/ADVANTAGE - Cpds. (I) are condensn. agents for the prodn. of peptides, beta-lactams, amides and esters. They are esp. suitable for use in automated peptide syntheses. Compared with known condensn. agents such as BOP and TBTU, cpds. (I) have improved solubility properties, e.g. 1.5 mol/l in DMF or dichloromethane, and are readily accessible from non-carcinogenic starting materials. Further, in use they give high prod. yield with low byprod. formation.