Muncy, Geissler, Olds & Lowe, P.C.
Method for synthesizing etelcalcetide or salts thereof
The present invention provides a method for synthesizing etelcalcetide or salts thereof, comprising the steps of: (a) synthesizing the D-amino acids in the formula (I) sequentially by Fmoc solid-phase synthesis, using a solid support as a starting material in solid phase peptide synthesis and sequentially synthesizing a D-form amino acid of formula (I) by Fmoc chemistry; deprotecting Fmoc group and acetylating the amino group to obtain a sequence A comprising protecting groups (PG) in the side chain of D-Cys and D-Arg; (b) removing the protecting group in the side-chain of D-Cys of the sequence A to form a sequence B; (c) disulfide formation at D-Cys of the sequence B by (PG)-L-Cys-OH to obtain a sequence C; (d) using a cleavage solution to remove the protecting groups of the sequence C to give etelcalcetide as formula (I). The present invention can shorten the steps and time for preparing Etelcalcetide.
CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO. LTD
C C C Y
C07K C07K C07K Y02P
inventional inventional inventional additional
Ya-Ling Chia-Sui Kwang-Chung Wei-Ssu Hui-Wen Kuang-Chan
Huang Kao Lee Wang Cheng Hsieh