- Synthesis method of enzalutamide
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The invention discloses a synthesis method of enzalutamide. According to the method, 4-amino-2-trifluoromethyl benzonitrile is adopted as an initial raw material, and the initial raw material, benzoyl isothiocyanate (a reaction product of ammonium thiocyanate and benzoyl chloride), methyl 2-methyl-2-chloropropionate and N-methyl-4-bromo-2-fluorobenzamide are sequentially subjected to a multi-step substitution reaction to obtain the enzalutamide. The synthesis method not only can guarantee the yield and the product quality, but also can protect the health and safety of personnel, is safe in production, and is suitable for industrial production.
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Paragraph 0020; 0036-0037
(2021/04/14)
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- A method for synthesizing graciousness mixed lu an
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The invention discloses a novel method for compounding enzalutamide, belongs to the technical field of pharmacy synthetic technology, and particularly relates to novel technology for compounding enzalutamide. Most known methods for compounding enzalutamide relate to use of highly toxic and mephitical thiophosgene and highly toxic oxobutyronitrile, and have relatively great difficulty for industrialization. According to the invention, non-toxic and harmless thiourea and an isobutyric acid derivative are used for a reaction to obtain a key parent nucleus of 5,5-dimethyl-2-thioketone imidazole-4-ketone, and therefore, thiophosgene and oxobutyronitrile are effectively avoided. The method has a mild reaction condition, is relatively high in yield, and therefore has a great industrial prospect.
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Paragraph 0044-0046
(2017/09/12)
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- Phenylimidazolidines having antiandrogenic activity
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A compound of the formula STR1 wherein R1 is --CN, --NO2 or halogen, R2 is --CF3 or halogen, --A--B-- is of STR2 X is --O-- or --S--, R3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted by at least one oxygen, nitrogen or sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A-B-- is STR3 X is oxygen, R3 is hydrogen and Y is oxygen or --NH--, R2 is --CF3 or halogen and R1 is --NO2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.
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- Phenylimidazolidines having antiandrogenic activity
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A compound of the formula STR1 wherein R 1 is --CN, --NO 2 or halogen, R 2 is --CF 3 or halogen, --A-B-- is of STR2 X is --O-- or --S--, R 3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF 3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH 2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted by at least one oxygen, nitrogen or sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A-B-- is STR3 X is oxygen, R 3 is hydrogen and Y is oxygen or --NH--, R 2 is --CF 3 or halogen and R 1 is --NO 2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.
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