4-Bbz-put
Chemical Name: 4-(4-Aminobutylaminomethyl)phenylboronic acid dihydrochloride
项目整合开发状态: Preclinical
项目研究机构: CNRS (Originator)
合成路线:The mono-Boc-protected diamine (II) was obtained by reaction of 1,4-diaminobutane (I) with Boc2O.Reductive alkylation of (II) to the benzylic amine (V) was carried out in a two-step procedure consisting in condensation of amine (II) with the formyl boronic ester (III) in the presence of molecular sieves,followed by reduction of the resultant imine (IV) with NaBH4.The N-Boc protecting group of (V) was then removed by acidic treatment,yielding diamine (VI).The title boronic acid was finally obtained by boronate ester exchange in (VI) with phenylboronic acid in a two-phase system.
📌 参考资料/链接:
参考文献标题:N'-Benzylpolyamines as vectors of boron and fluorine for cancer therapy and imaging: Synthesis and biological evaluation
文献作者:Martin,B.; Posseme,F.; Le Barbier,C.; Carreaux,F.; Carboni,B.; Seiler,N.; Moulinoux,J.P.; Delcros,J.G.
参考来源:J Med Chem 2001,44(22),3653