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Catalyst controlled diastereoselective N-alkylations of α-amino esters

✍ Scribed by Barry M. Trost; Trevor L. Calkins; Clements Oertelt; Jorge Zambrano


Publisher
Elsevier Science
Year
1998
Tongue
French
Weight
248 KB
Volume
39
Category
Article
ISSN
0040-4039

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✦ Synopsis


The design and synthesis of peptidomimetics constitutes one of the most important strategies for new drug discovery. N-Alkylated amino acid derivatives represent an interesting class. For example, the clinically


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✍ W. Russell Bowman; Daniel R. Coghlan 📂 Article 📅 1997 🏛 Elsevier Science 🌐 French ⚖ 853 KB

Monoalkylation of the a-amino group of or-amino acid derivatives can be facilitated using 2and 4-nitrophenylsulfonamide intermediates. The nitrophenylsulfonamides of a-amino esters can be alkylated using an equimolar amount of carbonate base and a variety of alkyl bromides. Ready removal of the nitr