Abstract:
The present invention is to provide a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzoic acid, 2,3,4-trifluoro-5-trifluoromethylbenzoic acid, esters thereof, which are useful as a starting material for synthesizing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzoic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.
Abstract:
The present invention is to provide a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzoic acid, 2,3,4-trifluoro-5-trifluoromethylbenzoic acid, esters thereof, which are useful as a starting material for synthesizing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzoic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.
Abstract:
Substituted trifluorobenzoic acids and esters thereof, useful as a starting material for the synthesis of quinolonecarboxylic acid compounds useful as medicines, antibacterial agents and antiviral agents, particularly 2,3,4-trifluoro-5-iodobenzoic acid, 2,3,4-trifluoro-5-trifluoromethylbenzoic acid and esters thereof; and processes for producing these compounds and further 2,4,5-trifluoro-3-iodobenzoic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.
Abstract:
The present invention relates to a benzobis(thiadiazole) derivative represented by the formula (1): wherein R represents a group containing at least one fluorine atom (with the proviso that fluorine atom (F) and trifluoromethyl group (-CF 3 ) are excluded), and m represents an integer of from 1 to 10.
Abstract:
The present invention relates to a benzobis(thiadiazole) derivative represented by the following general formula (1): wherein R 1 represents a linear or branched alkyl group, or any one of the groups of the following formula (2): wherein R represents a linear or branched alkyl group; R 2 represents a hydrogen atom; and R 3 represents a hydrogen atom, a linear or branched alkyl group, or any one of the groups of the formula (2); with the proviso that at least one of R 1 and R 3 represents any one of the groups of the formula (2); and two R 1 groups, two R 2 groups, and two R 3 groups may be the same as, or different from each other.
Abstract:
PURPOSE: To obtain 3-fluoro-4-chloro-6-aminobenzaldehyde (acetal) as a new compound capable of giving quinolines having antiallergic activity in high yield, thus useful as an intermediate for antiallergic agents. CONSTITUTION: This new compound is 3-fluoro-4-chloro-6-aminobenzaldehyde of formula I or a compound of formula II (R and R are each a 1-4C alkyl and may be bound to each other) (e.g. 3-fluoro-4-chloro-6-aminobenzaldehyde ethyleneacetal). The compound of formula I or formula II is obtained by catalyst hydrogen reduction of a compound of formula III [X is F; X is Cl; Y is formyl or an acetal group of the formula CH(OR )(OR )] in the presence of a platinum- or ruthenium-contg. catalyst in an organic solvent under pressure.
Abstract:
PURPOSE: To obtain 3-fluoro-4-chloro-6-nitrobenzaldehyde and its acetal which can give a quinoline in high yield and is useful as a synthetic intermediate for an antiallergic. CONSTITUTION: 3-Fluoro-4-chloro-6-nitrobenzaldehyde of formula I. The compound of formula I is obtained by nitrating 3-fluoro-4-chloro-benzaldehyde with the mixed acid. 3-Fluoro-4-chloro-6-nitrobenzaldehyde acetal of formula II is prepared by reaction of 3,4-dichlor-6-nitrobenzaldehyde acetal with an alkali metal fluoride in a polar solvent or by reaction of the compound of formula I with an aliphatic alcohol or an ortho-acid trialkyl ester in the presence of an acid catalyst.
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing a diaryl disulfide compound in high yield without requiring complicated operation by using an easily available reaction reagent. SOLUTION: The method for producing the diaryl disulfide compound represented by the formula: Ar-S-S-Ar (wherein, Ar is aryl or heteroaryl which may have a substituent) includes reacting an arylsulfonyl compound represented by the formula: Ar-SO 2 -L (wherein, Ar has the same meanings as the above; and L is a leaving group), a reducing agent of a bromide represented by the formula: M-Br (wherein, M is a metal ion, a quaternary ammonium ion or a phosphonium ion) or a bromonium ion, and sulfuric acid in the presence of an organic acid. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To produce a 2,4,5-trifluoro-3-iodobenzoic acid and its ester which are useful as a material for 2,4,5-trifluoro-3-trifluoromethyl benzoic acids used as a starting material for production of antimicrobial and antiviral agents, easily and at a high yield. SOLUTION: This 2,4,5-trifluoro-3-iodobenzoic acid of formula I (R is an alkyl, cycloalkyl or aralkyl) is produced by making a 2,4,5-trifluoroiodobenzoic acid of formula II with a N-iodosuccinimide of formula III in the presence of trifluoromethane sulfonic acid. Furthermore, a 2,4,5-trifluoro-3-iodobenzoic ester of formula IV is obtained by reaction of a reactant mixture that contains a compound of formula I with an alcohol of the formula of R-OH.
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing 2,4,5-trifluoro-3-iodobenzoic acid useful as a raw material for the production of 2,4,5-trifluoro-3- trifluoromethylbenzoic acid which is an important intermediate for synthesizing quinolone carboxylic acid compounds useful as medicines, antibacterial agents and antiviral agents. SOLUTION: A method for producing 2,3,4-trifluoro-3-iodobenzoic acid comprises reacting 3-amino-2,4,5-trifluorobenzoic acid with hydroiodic acid in the presence of sodium nitrite and a cuprous halide in a solvent.