Abstract：
Pyridyloxy-directed Ir(III)-catalyzed diacylmethylation of protected tyrosines was achieved with alkyl and (hetero)aryl sulfoxonium ylides, furnishing tyrosine-based unnatural amino acids in good yields. Furthermore, the late stage exemplification of the strategy was successfully accomplished in tyrosine-containing dipeptides, tripeptides and tetrapeptides in moderate yields. This methodology is distinguished by its site-selectivity, tolerance of sensitive functional groups, scalability, and retention of the chiral configuration for tyrosine motifs.
摘要：
用烷基和（杂）芳基亚砜叶立德实现了吡啶氧基定向的Ir（III）催化的受保护酪氨酸的二酰基甲基化，以高产率提供基于酪氨酸的非天然氨基酸。此外，该策略的后期示例在含酪氨酸的二肽中成功完成，三肽和四肽产量适中。这种方法的特点是它的网站选择性，敏感官能团的耐受性，可扩展性，和保留酪氨酸基序的手性构型。
