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项目整合精选>>>Bortezomib, MLN-341, DPBA, LDP-341, NSC-681239, PS-341, Velcade
Bortezomib, MLN-341, DPBA, LDP-341, NSC-681239, PS-341, Velcade
硼替佐米Chemical Name: 3-Methyl-1(R)-[N-(pyrazin-2-ylcarbonyl)-L-phenylalanylamino]butylboronic acid; N-(Pyrazin-2-ylcarbonyl)-L-phenylalanyl-L-boroleucine; N-[1(S)-[N-[1(R)-(Dihydroxyboryl)-3-methylbutyl]carbamoyl]-2-phenylethyl]pyrazine-2-carboxamide
CAS No. 179324-69-7
项目整合开发状态: Launched-2003
项目研究机构: Millennium (Proprietary), Millennium (Orphan Drug), ProScript (Originator), Ortho Biotech (Licensee), National Cancer Institute (Codevelopment)
合成路线:Pinanediol leucine boronate (I) was coupled with N-Boc-L-phenylalanine (II) in the presence of TBTU to afford the dipeptide boronate (III).Acid cleavage of the Boc protecting group of (III),followed by acylation of the resultant amine (IV) with 2-pyrazinecarboxylic acid (V),furnished amide (VI).Finally,deprotection of the boronic acid (VI) was accomplished by two-phase transesterification with isobutylboronic acid.
📌 参考资料/链接：
参考文献标题:Boronic ester and acid cpds.,synthesis and uses
文献作者:Adams,J.; Ma,Y.-T.; Stein,R.; Baevsky,M.; Grenier,L.; Plamondon,L.(ProScript,Inc.)
参考来源:JP 1998510245; US 5780454; US 6083903; WO 9613266
📄 详细内容
合成路线:Pinanediol leucine boronate (I) was coupled with N-Boc-L-phenylalanine (II) in the presence of TBTU to afford the dipeptide boronate (III).Acid cleavage of the Boc protecting group of (III),followed by acylation of the resultant amine (IV) with 2-pyrazinecarboxylic acid (V),furnished amide (VI).Finally,deprotection of the boronic acid (VI) was accomplished by two-phase transesterification with isobutylboronic acid.
参考文献标题:Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids
文献作者:Adams,J.; Behnke,M.; Chen,S.; Cruickshank,A.A.; Dick,L.R.; Grenier,L.; Klunder,J.M.; Ma,Y.T.; Plamondon,L.; Stein,R.L.
参考来源:Bioorg Med Chem Lett 1998,8(4),333
产品链接: CAS No. 179324-69-7››