2376-00-3Relevant academic research and scientific papers
NOVEL PHENYLALANINE DERIVATIVE
-
Page 74, (2008/06/13)
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.
METHOD FOR METAL-ORGANIC PRODUCTION OF ORGANIC INTERMEDIATE PRODUCTS BY MEANS OF ARYL LITHIUM-BASES
-
Page/Page column 14, (2010/02/06)
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.
Reagent-modulated optional site selectivities: The metalation of o-, m- and p-halobenzotrifluorides
Mongin,Desponds,Schlosser
, p. 2767 - 2770 (2007/10/03)
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.
2-[(2',6'-Disubstituted-phenyl)-imino]-imidazolidines and salts thereof
-
, (2008/06/13)
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
