An improved large scale procedure for the preparation of N-Cbz amino acids

作者：Pehere Ashok D; Abell Andrew D^*

来源：Tetrahedron Letters, 2011, 52(13): 1493-1494.

DOI：10.1016/j.tetlet.2011.01.102

• N-Cbz amino acids
• Synthesis
• Large scale
• Zofenopril

A simple and scalable method for the preparation of N-Cbz protected amino acids is presented which uses a mixture of aqueous sodium carbonate and sodium bicarbonate to maintain the appropriate pH during the addition of benzyl chloroformate. The method has been extended to other N-protections and is amenable to large scale preparation of an intermediate toward Zofenopril, an ACE inhibitor.

• 出版日期2011-3-30