- Brand new synthesis technology of lusutrombopag
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The invention relates to the field of organic chemistry, and especially relates to a brand new synthesis technology of lusutrombopag. The technology comprises the following steps: preparing an intermediate 3-(2-aminothiazolyl-4-yl)-2-methoxyacetophenone (4) from 2-methoxy-1,3-diacetylbenzene, reacting 3-(2-aminothiazolyl-4-yl)-2-methoxyacetophenone (4) with methyl (E)-ethyl-3-(2,6-dichloro-4-(chloroformyl)phenyl)-2-acrylate (5) to obtain a key intermediate methyl (E)-ethyl-3-(4-((4-(3-acetyl-2-methoxyphenyl)thiazolyl-2-yl)carbamoyl)-2,6-dichlorophenyl)-2-acrylate (6), carrying out catalytic reduction on the key intermediate, carrying out a halogenations reaction, and carrying out a hydrolysis reaction to obtain the target compound lusutrombopag. The technology has the advantages of easily available raw material, mild reaction conditions, simplicity in operation, good stability and activity of a catalyst, high total yield, and convenience for large-scale preparation and production of lusutrombopag.
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- PHARMACEUTICAL COMPOSITION CONTAINING OPTICALLY ACTIVE COMPOUND HAVING THROMBOPOIETIN RECEPTOR AGONIST ACTIVITY AND INTERMEDIATE THEREOF
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An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be
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(2010/06/11)
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