- Synthesis of trifluoromethylated α-hydroxy acids and their derivatives based on alkyl trifluoropyruvates
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The reactions of trifluoropyruvates with nitromethane and arylmagnesium bromides leading to trifluoromethyl-containing α-hydroxy acid esters were studied and various derivatives of the acids were obtained.
- Vasilyeva,Vorobyeva
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- Arylpiperidinopropanol and arylpiperazinopropanol derivatives and pharmaceuticals containing the same
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A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1to R4independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5represents H, optionally substituted alkyl, aryl, or aralkyl group, E1represents O, S, or —NR6, where R6represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2represents O, S, or —NR7, where R7represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1represents O or S, E2does not represent O or S, which has an action of suppressing the cytotoxic Ca2+overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.
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- Phenylbutanol derivatives and compositions containing them
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Phenylbutanol derivatives of the formula Z--C(CH3) (OH)--CH2 --Y wherein Z is 4-biphenyl or 4-phenoxyphenyl wherein the phenoxy group is unsubstituted or substituted by F, Cl or Br and Y is COOR2 or CH2 OR3 wherein R2 is H or alkyl of 1 to 6 carbon atoms and R3 is H or alkanoyl of 1 to 6 carbon atoms, and their physiologically acceptable salts, possess anti-inflammatory activity and are produced by (a) treating with a solvolyzing agent a compound of the formula Z--C(CH3) (OH)--CH2 --W or Z--CX(CH3)--CH2 --Y wherein W is a functionally modified carboxy or methylol group different from Y and X is Cl, Br or I or a functionally modified hydroxyl group; or (b) reducing a compound otherwise corresponding to a desired final product but having instead of one of the hydrogen atoms a group which can be reduced or replaced by a hydrogen atom; or (c) oxidizing a compound otherwise corresponding to a desired final product but lacking the tertiary hydroxyl group; or (d) converting a compound otherwise corresponding to a desired final product wherein Z is a 4-phenoxyphenyl group but having instead a 4--OH--, Cl--, Br-- or I-substituted phenyl group into a desired final product; or (e) diazotizing a compound otherwise corresponding to a desired final product wherein Z is a halogen-substituted 4-phenoxyphenyl group but having an --NH2 -substituted phenoxy group and reacting the resulting diazonium salt with a halogenating agent.
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