Solvent-Free Synthesis of Peptides

被引:164
作者
Declerck, Valerie [1 ]
Nun, Pierrick [1 ]
Martinez, Jean [1 ]
Lamaty, Frederic [1 ]
机构
[1] Univ Montpellier 2, CNRS, UMR 5247, UM1,UM2,IBMM, F-34095 Montpellier 5, France
关键词
ball-milling; peptides; peptide synthesis; solid-state reactions; solvent-free reactions; URETHANE N-CARBOXYANHYDRIDES; BETA-KETO-ESTERS; SOLID-STATE; AMINO-ACIDS; ASYMMETRIC-SYNTHESIS; KINETIC RESOLUTION; UNCAS; REAGENTS;
D O I
10.1002/anie.200903510
中图分类号
O6 [化学];
学科分类号
070301 [无机化学];
摘要
Chamical Equation Presentation A crush on sweetness! The coupling of a urethane-protected N-carboxyanhydride of an amino acid with another amino acid derivative under ball-milling conditions gives a protected dipeptide in very high yield (see scheme; PG: protecting group). The reaction takes place in the solid state. The synthesis was applied to the preparation of a tri peptide and the sweetener aspartame, without any organic solvent or purification. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:9318 / 9321
页数:4
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