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US 12,570,692 B2Granted
Oligopeptide linker intermediate and preparation method thereof
AssigneeMabplex International Co., Ltd.
InventorsLele Li, Changjiang Huang
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Abstract
The invention provides a new oligopeptide linker intermediate and a preparation method thereof. The preparation method of the oligopeptide intermediate is easily carried out under mild reaction conditions, and since almost no side reactions occur in the reaction, the method produces a high-purity product with fewer impurities and easy to be purified, achieving unexpected technical effects.
Claims2
A method for preparing the oligopeptide linker intermediate of formula (1), wherein the oligopeptide linker intermediate of formula (1) is obtained via the following reaction path:
- wherein the method comprises the following steps:
- 1) performing a condensation reaction between a carbonylation reagent, 2-(trimethylsilyl)ethanol and amino acid AA1 to obtain a 2-(trimethylsilyl)ethoxycarbonyl-amino acid condensate;
- 2) performing a condensation reaction between the 2-(trimethylsilyl)ethoxycarbonyl-amino acid condensate and amino acid AA2 to obtain a 2-(trimethylsilyl)ethoxycarbonyl-dipeptide condensate;
- and
- 3) performing a condensation reaction between the 2-(trimethylsilyl)ethoxycarbonyl-dipeptide condensate and p-aminobenzyl alcohol to obtain a 2-(trimethylsilyl)ethoxycarbonyl-dipeptide-p-aminobenzyl alcohol condensate;
- wherein the amino acid AA1 is valine, the amino acid AA2 is citrulline;
- and
- the carbonylation reagent is
5 more elements
Dependencies are inferred from the claim text.