- Making method of t-butyloxycarboryl-3-(hydroxymethyl)-[1,2,3]triazole[1,5-a]piperidine-6-amide
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The invention relates to a synthesis method of t-butyloxycarboryl-3-(hydroxymethyl)-[1,2,3]triazole[1,5-a]piperidine-6-amide. The technical problem that a suitable industrial synthesis method does not exist at present is mainly solved. The synthesis method is divided into the following seven steps of firstly making (2-chloro-5-nitropyridine) and t-butyl ethyl malonate react in a solvent tetrahydrofuran under the action of NaH to obtain a compound 2; obtaining a compound 3 from the compound 2 under the action of trifluoroacetic acid; afterwards, subjecting the compound 3 to a hydrogenation reaction under the catalysis of palladium carbon to obtain a compound 4; carrying out t-butyloxycarboryl protection on the compound 4 to obtain a compound 5; making the compound 5 act with p-ABSA (p-Acetamidobenzenesulfonyl Azide) under the action of DBU (1,8-Diazabicyclo[5,4,0]undec-7-ene) to obtain a compound 6; reducing the compound 6 in the tetrahydrofuran by lithium aluminium tetrahydride to obtain a compound 7; subjecting the compound 7 to catalytic hydrogenation under the catalysis of wet palladium carbon to obtain a final compound 8.
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- QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR INHIBITORS
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Compounds of formula (Ι') that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
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- INHIBITORS OF CYTOMEGALOVIRUS
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Compounds of Formula (I) wherein n, R1, R1A, R2, R4 and Z are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
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- INDAZOLECARBOXAMIDE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS
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This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such
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Page/Page column 25
(2008/06/13)
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- Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
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Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
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- EP4 RECEPTOR INHIBITORS TO TREAT RHEUMATOID ARTHRITIS
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The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin EP4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.
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