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A Short and Scalable Synthesis of Orthogonally Protected Bis(aminomethyl)malonic Acid: Access to Bioactive Macrocyclic Peptides
| Content Provider | Scilit |
|---|---|
| Author | Vetrichelvan, Muthalagu Bokkala, Vijayabhaskar Renganathan, Surendran Mathur, Arvind Rampulla, Richard Gupta, Anuradha |
| Copyright Year | 2017 |
| Description | A short and scalable process for the preparation of multi-gram quantities of orthogonally protected bis(aminomethyl)malonic acid in good yield from readily available starting material is described. These orthogonally protected amino acids are important building blocks to make peptides based drugs, glycoconjugates, and in the total synthesis of peptide natural products. The newly developed route has only six steps with an overall yield of 27%, which involves nucleophilic attack of a malonate on an imide as one of the key steps. |
| Related Links | http://pdfs.semanticscholar.org/fd05/d1d668b507b6f445c9b3b8df7a98209731bd.pdf http://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-0036-1588505.pdf |
| Ending Page | 5044 |
| Page Count | 6 |
| Starting Page | 5039 |
| ISSN | 00397881 |
| e-ISSN | 1437210X |
| DOI | 10.1055/s-0036-1588505 |
| Journal | Synthesis |
| Issue Number | 22 |
| Volume Number | 49 |
| Language | English |
| Publisher | Georg Thieme Verlag KG |
| Publisher Date | 2017-08-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Synthesis Organic Chemistry Macrocyclic Peptides Orthogonally Protected Amino Acid Gram Scale Synthesis Improved Process Benzyl Ethyl Malonate |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Catalysis |
