- Preparation method of lifitegrast intermediate
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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.
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Paragraph 0047-0048
(2020/08/09)
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- Intensified biocatalytic production of enantiomerically pure halophenylalanines from acrylic acids using ammonium carbamate as the ammonia source
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An intensified, industrially-relevant strategy for the production of enantiopure halophenylalanines has been developed using the novel combination of a cyanobacterial phenylalanine ammonia lyase (PAL) and ammonium carbamate reaction buffer. The process boasts STYs up to >200 g L-1 d-1, ees ≥ 98% and simplified catalyst/reaction buffer preparation and work up.
- Weise, Nicholas J.,Ahmed, Syed T.,Parmeggiani, Fabio,Siirola, Elina,Pushpanath, Ahir,Schell, Ursula,Turner, Nicholas J.
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p. 4086 - 4089
(2016/07/06)
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- LFA-1 INHIBITOR AND POLYMORPH THEREOF
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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.
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Paragraph 00120; 00121; 00122; 00123; 00124; 00125
(2014/02/16)
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- Discovery and development of potent LFA-1/ICAM-1 antagonist SAR 1118 as an ophthalmic solution for treating dry eye
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LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.
- Zhong, Min,Gadek, Thomas R.,Bui, Minna,Shen, Wang,Burnier, John,Barr, Kenneth J.,Hanan, Emily J.,Oslob, Johan D.,Yu, Chul H.,Zhu, Jiang,Arkin, Michelle R.,Evanchik, Marc J.,Flanagan, W. Mike,Hoch, Ute,Hyde, Jennifer,Prabhu, Saileta,Silverman, Jeffrey A.,Wright, Jasmin
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supporting information; scheme or table
p. 203 - 206
(2012/05/04)
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- MACROCYCLIC INHIBITORS OF HEPATITIS C PROTEASE
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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
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Page/Page column 56
(2009/10/09)
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- SULFONAMIDE COMPOUNDS
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Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.
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Page/Page column 20
(2010/10/20)
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