Racemisierungsfreies Verfahren zum Aufhängen von Aminosäuren auf einer Festphase

摘要

This invention pertains to amino acids attached to a solid support in a racemization free manner and to a method of covalently linking amino acids to solid supports for use in solid phase peptide syntheses, through a compound of the formula: wherein Z is an N alpha protecting group; B is one or more amino acids having protected or unprotected side chains; R1 and R2 are the same or different and are selected from the group consisting of hydrogen, a linear or branched, saturated or unsaturated alkyl, aryl and benzyl; A is a substituted or unsubstituted aromatic ring; Y is a hydrocarbon chain having a linear or branched, saturated or unsaturated alkyl, aryl or aralkyl which may be linked to A through an ether linkage; D is an oxygen or -NH- which may be linked to a spacer selected from the group consisting of one or more natural and unnatural amino acids or hydrocarbon chain having a linear or branched, saturated or unsaturated alkyl, aryl or aralkyl group, the spacer being linked to the carbonyl through an oxygen or -NH- linkage; and SS is a solid support which is bound to the carbonyl group through D.