Daniels Blake E, Stivala Craig E
Discovery Chemistry, Genentech, Inc. 1 DNA Way South San Francisco CA 94080 USA
RSC Adv. 2018 Jan 16;8(6):3343-3347. doi: 10.1039/c7ra13479g. eCollection 2018 Jan 12.
A solid-phase synthesis of α-aminoboronic acid peptides using a 1-glycerol polystyrene resin is described. Standard Fmoc solid-phase peptide chemistry is carried out to construct bortezomib and ixazomib. This approach eliminates the need for liquid-liquid extractions, silica gel column chromatography, and HPLC purifications, as products are isolated in high purity after direct cleavage from the resin.
描述了一种使用1-甘油聚苯乙烯树脂进行α-氨基硼酸肽的固相合成方法。采用标准的Fmoc固相肽化学方法来构建硼替佐米和伊沙佐米。这种方法无需液-液萃取、硅胶柱色谱和HPLC纯化,因为从树脂上直接切割后,产物能以高纯度分离出来。