Concise Synthesis of Sibrafiban and Lamifiban,Two Non-Peptide Fibrinogen Receptor (GP Ilb/Illa) Antagonists

摘要

The total synthesis of the non-peptide fibrinogen receptor antagonists, sibrafiban (1)(Ro 48-3657) and lamifiban (2)(Ro 44-9883), is described. Both contain 4-hydroxypiperidine unit and the same solid-phase synthesis method was used as a key step. Connection of a secondary alcohol to the DHP-resin,followed by iterative saponification and coupling sequences,provided novel drugs.