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US 8,013,117 B2Granted
Solution-phase synthesis of leuprolide and its intermediates
AssigneeNanokem Co., Ltd.
InventorsDaniel Kadzimirsz, Gerhard Jas, Volker Autze
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Abstract
A process for producing a nonapeptide leuprolide and an intermediate N-protected oligopetides, wherein at least one peptide bond of the compound is formed by reacting an activated carboxylic acid and an amine component in a continuous flow.
Claims18
A process comprising:
- producing the nonapeptide leuprolide or an N-protected intermediate oligopeptide thereof of formula 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl (SEQ ID NO:
- 6), by:
- forming at least one peptide bond of the compound by reacting an activated carboxylic acid and an amine component in a continuous flow, and
- feeding said activated carboxylic acid and said amine component, each in a continuous flow, simultaneously into a reaction system.
1 more element
Dependencies are inferred from the claim text.