Scinopharm Taiwan, Ltd.

Ming-Chih Wu

Tsung-Yu Hsiao

Tsung-Cheng Hu

YuanChang Huang

Wen-Wei Lin

Hsin-Che Huang

The present invention provides improved processes for purifying semaglutide or liraglutide. Semaglutide or liraglutide is purified via two sequential RP-HPLC purifications followed by a salt-exchange step, where a pH is kept constant in the first and second purification steps. In particular, the processes utilize a halogenated solvent in a sample preparation step, which provides better solubility and an environment suitable for decarboxylation for crude semaglutide or liraglutide prior to a RP-HPLC purification.

Process for purifying semaglutide and liraglutide

The present invention provides improved processes for purifying liraglutide. Liraglutide is purified via two sequential RP-HPLC purifications followed by a salt-exchange step, where a pH is kept constant in the first and second purification steps. In particular, the processes utilize a halogenated solvent in a sample preparation step, which provides better solubility and an environment suitable for decarboxylation for crude liraglutide prior to a RP-HPLC purification.

Process for purifying liraglutide

Crystalline form S1 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 10.7&#xb1;0.2, 16.2&#xb1;0.2, 19.9&#xb1;0.2, 22.1&#xb1;0.2, 24.7&#xb1;0.2, and 25.9&#xb1;0.2 degrees two-theta, crystalline form S2 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 16.4&#xb1;0.2, 24.9&#xb1;0.2, and 26.2&#xb1;0.2 degrees two-theta, and processes of making thereof are provided.

Crystal forms of lifitegrast

The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.

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Tainan, Taiwan

Ming-Chih Wu