Volume 31, Issue 12
Isocyclic Compounds
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ChemInform Abstract: A Convenient Method for the N-Acylation and Esterification of Hindered Amino Acids: Synthesis of Ultra Short Acting Opioid Agonist, Remifentanil.

Mark J. Coleman

Mark J. Coleman

Chem. Dev. Div., Glaxo Wellcome Res. Dev., Stevenage, Hertfordshire SG1 2NY, UK

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Michael D. Goodyear

Michael D. Goodyear

Chem. Dev. Div., Glaxo Wellcome Res. Dev., Stevenage, Hertfordshire SG1 2NY, UK

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David W. S. Latham

David W. S. Latham

Chem. Dev. Div., Glaxo Wellcome Res. Dev., Stevenage, Hertfordshire SG1 2NY, UK

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Andrew J. Whitehead

Andrew J. Whitehead

Chem. Dev. Div., Glaxo Wellcome Res. Dev., Stevenage, Hertfordshire SG1 2NY, UK

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First published: 09 June 2010

Abstract

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ChemInform Abstract

An easily performed sequence allows the conversion of α-amino acids of type (I) to N-acylamino acid esters (IV), isolated as oxalates. Derivative (IVa) is a valuable precursor of remifentanil (VII).

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