首页> 外国专利> DIPEPTIDE BORONIC ACID CONTAINING Β-AMINO ACID AND CARBOXYLIC ACIDS, ITS ESTER COMPOUNDS, PREPARATION METHOD AND USE THEREOF

DIPEPTIDE BORONIC ACID CONTAINING Β-AMINO ACID AND CARBOXYLIC ACIDS, ITS ESTER COMPOUNDS, PREPARATION METHOD AND USE THEREOF

机译:含α-氨基酸和羧酸的双硼酸硼酸酯,其酯化合物,制备方法及其用途

摘要

Dipeptide boronic acid containing β-amino acid and carboxylic acids, its ester compounds, its preparation method and its use are provided. This compound has the structure of formula I, wherein R1 is substituted or unsubstituted C1-C10 alkyl, C3-C6 cycloalkyl or heterocyclic alkyl, phenyl, naphthyl, or indolyl; R2 is substituted or unsubstituted C1-C10 alkyl, C3-C6 cycloalkyl or heterocyclic alkyl, benzyl, menaphthyl, or indolmethyl; Z1 and Z2 are hydroxy, C1-C10 alkyl, C1-C10 alkoxy or aryloxy, independently; or B, Z1 and Z2 form together N-, S- or O-containing heterocycle; Pg is substituted or unsubstituted C1-C10 alkylacyl, C1-C10 alkoxyacyl, aromatic acyl, or N-, S- or O-containing heterocyclic acyl. The present compounds have application in the preparation of proteasome inhibitor or antitumor agent.
机译:提供了含有β-氨基酸和羧酸的二肽硼酸,其酯化合物,其制备方法和用途。该化合物具有式I的结构,其中R 1 是取代或未取代的C1-C10烷基,C3-C6环烷基或杂环烷基,苯基,萘基或吲哚基; R 2 是取代或未取代的C1-C10烷基,C3-C6环烷基或杂环烷基,苄基,甲萘基或吲哚甲基; Z 1 和Z 2 分别是羟基,C1-C10烷基,C1-C10烷氧基或芳氧基;或B,Z 1 和Z 2 一起形成含N,S或O的杂环; Pg是取代或未取代的C1-C10烷酰基,C1-C10烷氧基,芳族酰基或含N-,S-或O的杂环酰基。本发明化合物可用于制备蛋白酶体抑制剂或抗肿瘤剂。

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