N-Benzyl-Protection of Amino Acid Derivatives by Reductive Alkylation with α-Picoline-Borane
作者:Tsutomu Yokomatsu、Yasushi Kawase、Takehiro Yamagishi、Teruo Kutsuma、Tadashi Kataoka、Kimio Ueda、Takeo Iwakuma、Tadashi Nakata
DOI:10.1055/s-0029-1218707
日期:2010.5
derivatives with a benzyl group by reductive alkylation of amino acid derivatives with α-picoline-borane is described. Amino acid esters or amino alcohols were treated with aryl aldehydes in methanol/acetic acid in the presence of α-picoline-borane to give N-benzyl-protected amino acid derivatives in good yields. amino acid esters - amino alcohols - benzylation - protecting groups - reductions
描述了一种方便的方法,该方法通过用α-甲基吡啶-硼烷对氨基酸衍生物进行还原性烷基化来用苄基对氨基酸衍生物进行N-保护。在α-甲基吡啶硼烷的存在下,用芳基醛在甲醇/乙酸中处理氨基酸酯或氨基醇,以高收率得到N-苄基保护的氨基酸衍生物。 氨基酸酯-氨基醇-苄基化-保护基-还原