PSEUDO PROLINE DIPEPTIDES

Disclosed is a three step process for the manufacture of pseudo proline dipeptides of the formula (I) wherein R1 is a side chain of an alpha amino acid , R2 is an amino protecting group and R3 and R4 are independently selected from hydrogen or C1-4-alkyl, R5 is hydrogen or methyl starting from an am...

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Bibliographic Details
Main Authors SANDRA WELZ, THOMAS AMMANN, KLAUS-JUERGEN WOLTER, BERND THERN, STEPHAN GOETZOE
Format Patent
LanguageEnglish
Spanish
Published 19.12.2008
Subjects
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
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Summary:Disclosed is a three step process for the manufacture of pseudo proline dipeptides of the formula (I) wherein R1 is a side chain of an alpha amino acid , R2 is an amino protecting group and R3 and R4 are independently selected from hydrogen or C1-4-alkyl, R5 is hydrogen or methyl starting from an amino acid derivative of the formula (II) wherein R1 and R2 are as above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry. Se da a conocer un proceso de tres pasos para la manufactura de dipéptidos de pseudo-prolina de la fórmula (I) en donde R1 es una cadena lateral de un aminoácido alfa, R2 es un grupo protector de amino y R3 y R4 se seleccionan independientemente de hidrógeno o alquilo de 1 a 4 átomos de carbono, R5 es hidrógeno o metilo partiendo de un derivado de aminoácido de la fórmula (II) en donde R1 y R2 son como se describiera anteriormente. Los dipéptidos de pseudo-prolina se pueden utilizar como grupos protectores reversibles para Ser, Thr y Cys y de esta manera son herramientas versátiles en la química de péptidos.
Bibliography:Application Number: MX20080015723