Efficient Preparation of Aminoxyacyl Amides, Aminoxy Hybrid Peptides, and α-Aminoxy Peptides
作者:Alan R. Katritzky、Ilker Avan、Srinivasa R. Tala
DOI:10.1021/jo901612j
日期:2009.11.20
N-(Pg-α-aminoxy acids) 1a−g are converted to N-(Pg-α-aminoxyacyl)benzotriazoles 2a−g, which react under mild conditions with amines, α-amino acids/α-dipeptides, and α-aminoxy acids to give aminoxyacyl amides 3a−g, (3e+3e′), and (3g+3g′), aminoxy hybrid peptides 4a−h, (4a+4a′), 6a−d, 9a−e, (9a+9a′), and (9b+9b′), and α-aminoxy peptides 10a,b in good yields without racemization.
将N-(Pg-α-氨氧基酸)1a - g转化为N-(Pg-α-氨氧基酰基)苯并三唑2a - g,使其在温和条件下与胺,α-氨基酸/α-二肽和α-氨氧基酸生成氨氧基酰基酰胺3a - g,(3e + 3e')和(3g + 3g'),氨氧基杂合肽4a - h,(4a + 4a'),6a - d,9a - e,(9a + 9a')和(9b + 9b'),以及α-氨氧基肽10a,b的产量高,没有消旋作用。