82278-73-7Relevant articles and documents
Preparation method of lifitegrast intermediate
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Paragraph 0047-0048, (2020/08/09)
The invention relates to a preparation method of a lifitegrast intermediate. The preparation method is implemented by the following route, has the advantages of short synthesis route, high yield and high safety, and is simple and convenient to operate and suitable for industrial production. According to the preparation method, a compound II reacts with metal zinc in an organic solvent to generatean organic zinc reagent, a compound I carries out a coupling reaction with the organic zinc reagent, a palladium reagent and a phosphorus ligand to obtain a compound III, and Boc protecting groups ofthe compound III are removed to obtain a compound IV, wherein R1 and R2 groups are respectively and independently selected from methyl, ethyl, vinyl, n-propyl, isopropyl, propenyl, propynyl, cyclopropyl, n-butyl, isobutyl, tert-butyl, butenyl, cyclobutyl, n-pentyl, iso-pentyl, cyclopentyl, n-hexyl, cyclohexyl, phenyl and benzyl.
LFA-1 INHIBITOR AND POLYMORPH THEREOF
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Paragraph 00120; 00121; 00122; 00123; 00124; 00125, (2014/02/16)
Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.
MACROCYCLIC INHIBITORS OF HEPATITIS C PROTEASE
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Page/Page column 56, (2009/10/09)
The invention provides compounds inhibitory to the Hepatitis C viral protease, compositions and combinations including the compounds, methods of treatment of conditions wherein inhibition of the Hepatitis C viral protease is medically indicated, and metho