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.
Bibliographical noteFunding Information:
We thank Dr. Vinayak Gore (Mylan India Private Limited) for carrying out the large scale reactions. The authors acknowledge the financial support of an ARC DP grant (A.D.A.) and the University of Adelaide for an AFSI scholarship to A.D.P.
- Large scale
- N-Cbz amino acids