- NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
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An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
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Paragraph 0828; 0829
(2018/09/08)
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- Synthesis method of 3-bromine-7-hydroxyquinoline
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The invention provides a synthesis method of 3-bromine-7-hydroxyquinoline. The synthesis method of the 3-bromine-7-hydroxyquinoline includes the following steps that 1, 7-hydroxyquinoline is dissolvedin solvent, trifluoromethanesulfonic anhydride is added, and low temperature reaction is carried out to obtain quinoline-7-trifluoromethanesulfonate, wherein the molar ratio of the 7-hydroxyquinolineto the trifluoromethanesulfonic anhydride is 1:(1-1.5); 2, the quinoline-7-trifluoromethanesulfonate obtained in step 1 is dissolved in solvent, N-bromosuccinimide is added, and after reaction, 3-bromoquinoline-7-trifluoromethanesulfonate is obtained; 3, the 3-bromoquinoline-7-trifluoromethanesulfonate obtained in step 2 is hydrolyzed under an alkaline condition to obtain the 3-bromine-7-hydroxyquinoline. According to the synthesis method of the 3-bromine-7-hydroxyquinoline, the raw materials are stable and non-toxic, the synthesis technology is simple, and the yield is high.
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Paragraph 0037; 0038; 0051
(2018/09/20)
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