89315-56-0Relevant articles and documents
Preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline
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Paragraph 0019; 0024; 0026; 0036-0039; 0048-0049, (2021/02/06)
The invention provides a preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline. The preparation method comprises the following steps: preparing a compound A by taking 3, 5-dichlorobenzoic acid as a raw material; preparing a compound B from the compound A; preparing a compound C from the compound B; preparing a compound D from the compound C; and obtaining a white solid 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline from the compound D. The preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline provided by the invention has the advantages of high product purity and high product yield.
Synthesis method of lifitegrast intermediate 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline
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, (2020/05/05)
The invention discloses a synthesis method of a lifitegrast intermediate 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline, wherein the synthesis method comprises the steps: by using 2,4-dichlorobenzaldehyde as a starting material, carrying out nitro-alcohol co
Discovery and development of potent LFA-1/ICAM-1 antagonist SAR 1118 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
supporting information; scheme or table, p. 203 - 206 (2012/05/04)
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.