- METHOD FOR METAL-ORGANIC PRODUCTION OF ORGANIC INTERMEDIATE PRODUCTS BY MEANS OF ARYL LITHIUM-BASES
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The invention relates to a method for the production of substituted aromatic compounds by producing lithium arylene and by reacting it with suitable electrophiles. The method comprises the following steps (step 1); an aryl lithium compound ( auxiliary base'') is initially produced by reacting a halogen aromatic compound with lithium metal; said compound is subsequently (step 2) reacted for deprotonation of the aromatic substrate in order to form the corresponding lithium aromatic compound which is subsequently (step 3) reacted with a corresponding electrophile to form the desired substituted aromatic compound, see page 2 of the description.
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Page/Page column 14
(2010/02/06)
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- NOVEL PHENYLALANINE DERIVATIVE
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The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin.
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- Reagent-modulated optional site selectivities: The metalation of o-, m- and p-halobenzotrifluorides
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Chloro(trifluoromethyl)benzenes and bromo(trifluoromethyl)benzenes undergo deprotonation at a position adjacent to the single halogen substituent when treated with alkyllithiums (at -75°C) and, respectively, lithium 2,2,6,6-tetramethylpiperidide (at -100°C) in tetrahydrofuran. Positional ambiguities, if existing, can be exploited to establish optional site selectivities. Thus, butyllithium reacts with 1-chloro-3-(trifluoromethyl)benzene under hydrogen/metal interconversion at the 2-position whereas sec-butyllithium attacks exclusively the 6-position. The latter mode of regioselectivity is also exhibited by 1-bromo-3-(trifluoromethyl)benzene in the presence of lithium 2,2,6,6-tetramethylpiperidide, only 2-bromo-4-(trifluoromethyl)phenyllithium being produced. 2-Bromo-6-(trifluoromethyl)phenyllithium is directly inaccessible, but is formed when 2-bromo-3-(trifluoromethyl)phenyllithium, generated at -100°C, is allowed to isomerize at -75°C.
- Mongin,Desponds,Schlosser
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p. 2767 - 2770
(2007/10/03)
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- 2-[(2',6'-Disubstituted-phenyl)-imino]-imidazolidines and salts thereof
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Compounds of the formula STR1 wherein Z is 2-ETHYL-6-METHYL-PHENYL, 2,6-di-trifluoromethyl-phenyl, 2-chloro-6-trifluoromethyl-phenyl or 2-fluoro-6-trifluoromethyl-phenyl, And non-toxic, pharmacologically acceptable acid addition salts thereof; the compoun
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