- Novel isomerization method of acitretin
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The invention belongs to the field of drug synthesis and research, and particularly relates to an isomerization catalyst which is a palladium-carbon composite catalyst and is a mixture of palladium-carbon and triphenylphosphine, and the molar ratio of the palladium-carbon to the triphenylphosphine is 1 to (1-10). The invention further provides a novel isomerization method of acitretin. The isomerization catalyst is adopted to perform an isomerization reaction, so that an isomer 11-cis,13-trans-acitretin in the mixture can be effectively converted into a medicinal all-trans acitretin, materialwaste is avoided, the prepared acitretin product is high in purity, the palladium-carbon catalyst can be recovered by adopting a simple method and can be reused, the product cost is reduced, the concentration of heavy metal ions in wastewater is low, the environmental pollution is reduced, and the process is environmentally friendly.
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Paragraph 0057; 0058; 0058
(2018/10/19)
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- PROCESS FOR PREPARATION OF ACITRETIN
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The present invention provides a process for preparation of {(2E,4E,6E,8E)-9-(4-methoxy-2,3,6- trimethyl)phenyl-3,7-dimethyl-nona-2,4,6,8}tetraenoate, an acitretin intermediate of formula (VI) with trans isomer ≥97%, comprising of reacting 3-formyl-crotonic acid butyl ester of formula (V), substantially free of impurities, with 5-(4-methoxy-2,3,6-trimethylphenyl)-3- methyl-penta-2,4-diene-l-triphenyl phosphonium bromide of formula (IV) and isolating resultant compound of formula (VI), treating the filtrate with iodine for isomerization of the undesired cis intermediate and finally obtaining acitretin (I), with desired trans isomer ≥97%.
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- 9-Phenyl-nonate traene compounds
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Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.
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