Patent classifications
C07C227/30
5-SUBSTITUTED-5-HYDROXY-5-ARYL-3-OXO-PENTANOATE DERIVATIVES AND THEIR ENANTIOPURE FORMS
The present invention relates to novel tertiary alcohol derivatives substituted with aryl and trifluoromethyl, and optical isomers thereof. In addition, the present invention also relates to methods for the preparation and use as enantiomer recognition agent thereof. The present invention provides pharmaceutical composition and use as therapeutically active substance thereof.
PROCESS FOR MAKING MIXTURES OF CHELATING AGENTS
Process for making a chelating agent according to the general formula (I), R.sup.1CH(COOX.sup.1)N(CH2COOX.sup.1).sub.2 wherein R.sup.1 is selected from hydrogen, C.sub.1-C.sub.4-alkyl, phenyl, benzyl, CH.sub.2OH, and CH.sub.2CH.sub.2COOX.sup.1, X.sup.1 is (M.sub.H.sub.1-), M being selected from alkali metal, x is in the range of from 0.6 to 1, said process comprising the following steps: (a) providing a solid, a slurry or a solution of a compound according to general formula (II a) R.sup.1CH(COOX.sup.2)N(CH.sub.2CN).sub.2 wherein X.sup.2 is (M.sub.yH.sub.1-y), M being selected from alkali metal, y is in the range of from zero to 1, (b) contacting said solid or slurry or solution with an aqueous solution of alkali metal hydroxide, wherein the molar ratio of alkali metal ions to nitrile groups is in the range of from 0.6:1 to 0.95:1, (c) reacting said compound according to general formula (II a) with said alkali metal hydroxide.
Axially chiral N-(2-acylaryl)-2-[5,7-dihydro-6h-dibenzo[c,e]azepin-6-yl] acetamide compound and chirality interconversion method of a-amino acid using the same
An object of the present invention is to provide a method for producing an optically active amino acid in high yield and in a highly enantioselective manner, which method has fewer restrictions on the material that can be used as the substrate, and to provide, among others, a compound useful as a chiral auxiliary for the method. The present invention provides an N-(2-acylaryl)-2-[5,7-dihydro-6H-dibenzo[c,e]azepin-6-yl]acetamide compound represented by Formula (1): ##STR00001##
or a salt thereof, or a metal complex represented, by Formula (3): ##STR00002##
Axially chiral N-(2-acylaryl)-2-[5,7-dihydro-6h-dibenzo[c,e]azepin-6-yl] acetamide compound and chirality interconversion method of a-amino acid using the same
An object of the present invention is to provide a method for producing an optically active amino acid in high yield and in a highly enantioselective manner, which method has fewer restrictions on the material that can be used as the substrate, and to provide, among others, a compound useful as a chiral auxiliary for the method. The present invention provides an N-(2-acylaryl)-2-[5,7-dihydro-6H-dibenzo[c,e]azepin-6-yl]acetamide compound represented by Formula (1): ##STR00001##
or a salt thereof, or a metal complex represented, by Formula (3): ##STR00002##