摘要:
The present invention relates to an environmentally benign process for preparation of (+)2-(4-chlorophenyl)-3-methyl butanoic acid (+ CPA) from its racemic acid, using optically active arylamines like (-) PEA in hydrophilic/hydrophobic organic solvents like butanol, propanol etc. as aqueous mixtures, separating the desired (+) CPA salt, mother liquor by filtration and refining the (+) CPA salt in the same solvent system as used for resolution, recovering the desired acid in high optical purity by extracting with aqueous mineral acid. The mother liquor is concentrated under vacuum and extracted with aqueous mineral acid to obtain undesired (-) CPA which was recovered and recycled after racemization. The aqueous mineral acid layer thus obtained is mixed with corresponding aqueous mineral acid layer obtained from (+) CPA recovery and extracted with aqueous caustic lie solution to recover the optically active amine used for resolution. Thus the method described effectively provides a process for recovery and recycle of the undesired (-) CPA, optically active amine, besides obtaining the desired (+) CPA in high optical purity.
摘要:
Novel halophenyl derivatives of the general formula (I), wherein R1 is halogen, a leaving group or 1H-1,2,4-triazol-l-yl and R2 is ethynyl or carboxy, X1 is halogen and X?2 and X3¿ are each independently hydrogen or halogen, and their manufacture are described. They are intermediates for manufacturing azole derivatives of the general formula (V) which are valuable medicaments useful for treating systemic mycoses.
摘要:
Verfahren zur Herstellung von Phenylessigsäurederivaten der allgemeinen Formel (I) durch Umsetzung von Benzylchloriden der allgemeinen Formel (II) mit einer Verbindung der allgemeinen Formel R 6 OH und mit Kohlenmonoxid in einem dipolar aprotischen Lösungsmittel in Gegenwart eines Katalysators, der mindestens eine Verbindung eines Übergangsmetalls der VIII. Nebengruppe des Periodensystems enthält, wobei R 1 , R 2 , R 3 , R 4 , und R 5 unabhängig voneinander für folgende Reste stehen: ein Wasserstoff oder Fluoratom;
ein CH 2 CI-Rest; eine HO 2 CCH=CH-, NC- oder CF 3 -Gruppe; einen Alkyl-, Alkoxy-, oder Acyloxyrest, mit jeweils 1 bis 18 Kohlenstoffatomen; oder einen C 6 -C 18 -Aryloxy, Aryl- oder Heteroarylrest, wobei als Heteroatome 1 bis 3 Atome der Gruppe O, N und/oder S vorhanden sind; einen R 8 2 P(=O)-, R 9 C(=O)-, R 9 OC(=O)-, R 9 OC(=O)CH=CH-, R 10 C(=O)-, R 10 OC(=O)-, R 10 OC(=O)CH=CH-, oder R 10 2 P(=O)-Rest, worin R 8 einen C 1 -C 4 -Alkylrest, R 9 einen C 1 -C 18 -Alkylrest oder Wasserstoff und R 10 einen C 6 -C 18 -Arylrest darstellen; oder worin mindestens zwei der Reste R 1 , R 2 , R 3 , R 4 , und R 5 untereinander verknüpft sind und mindestens einen aliphatischen oder aromatischen Ring mit 5 bis 18 C-Atomen bilden; R 6 steht für Wasserstoff oder einen C 1 -C 18 -Alkyl- oder C 6 -C 18 -Arylrest.
摘要:
A method of resolving d- and I-isomers of an α-arylpropionic acid, wherein the isomers are enantiomers. The method involves forming an ammonium salt of the α-arylpropionic acid, then dissolving in a solvent the ammonium salt, and a chiral agent capable of reacting with the ammonium salt of at least one of the isomers. The reaction product of the chiral agent and the ammonium salt of the one of the isomers can subsequently be purified, then separated into the chiral agent and the isomer.
摘要:
Described are drugs for the treatment of painful and/or inflammatory conditions with flurbiprofen, the previously separated enantiomers of flurbiprofen being combined in the ratio 99.5-0.5 % to 0.5-99.5 % and processed with the usual pharmaceutical vehicles and additives to give drugs. For pain, or chronic conditions in which pain is a dominant factor, the mixture of enantiomers contains 50-99.5 %, preferably 60-95 %, of R(-)-fluorbiprofen and for inflammations, or chronic conditions in which inflammation is a dominant factor, the mixture contains 50-99.5 %, preferably 60-95 %, of S(+)-flurbiprofen.
摘要:
An α-substituted phenylacetic acid derivative useful as an agricultural fungicide, represented by general formula (I), or a salt thereof, a process for producing the same, an intermediate for the production thereof, and an agricultural fungicide containing the same as the active ingredient, wherein R 1 represents halogen, alkyl, OH, alkylthio, alkylsulfinyl, alkylsulfonyl, amino or nitro; Q represents aryl, heterocycle, mono- or disubstituted methyleneamino, (substituted amino-)methyl, alkyl, alkenyl, alkynyl, substituted carbonyl or substituted sulfonyl; X represents hydrogen, halogen, alkyl or OH; Y represents OH, alkylthio or amino; Z represents oxygen or sulfur; M represents oxygen, S(O)i (i being 0, 1 or 2), NR 2 (R 2 being hydrogen, alkyl or acyl) or a single bond; and n represents 0, 1 or 2.