Abstract:
The invention concerns a method for preparing substituted benzyl bromides of general formula (I), wherein at least one substituent R represents an electroattractive group, such as fluorine, chlorine, bromine, C1-C4 alkoxycarbonyl, cyano or nitro, and the remaining R substituents represent hydrogen or methyl, by bromination of substituted toluenes of general formula (II) with a bromination agent at temperatures from 20 to 95 DEG C.
Abstract:
The invention relates to 3-cyano-2,4,5-trifluoro-benzoyl fluoride and intermediate products for the production thereof and a method for the production of 3-cyano-2,4,5-trifluoro-benzoyl fluoride starting from 5-fluoro-1,3-xylol (VIII), which is chlorinated twice in the presence of a catalyst with ionic conditions in the nucleus to obtain 2,4-dichloro-5-fluoro-1,3-dymethylbenzol (VII), which is then chlorinated with radical conditions in the side chains to obtain 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethyl benzol (VI), which is subsequently saponified by the optionally isolatable 2,4-dichloro-5-fluoro-3-dichloromethyl benzoic acid (V) to obtain 2,4-dichloro-5-fluoro-3-formyl-benzoic acid (IV) whose aldehyde group is converted to 2,4-dichloro-5-fluoro-3-N-hydroxyiminomethyl-benzoic acid (III), whereupon water is eliminated using an acid chloride while at the same time converting the carboxyl group into a chlorocarbonyl group to obtain nitrile 2,4-dichloro-3-cyano-5-fluoro-benzoyl-chloride (II), which is finally subjected to a fluorine/chlorine exchange.
Abstract:
Methods of making AF4 using novel reducing agents that result in reduced cost. Low dilution technology may be used to provide AF4 in substantially improved yields. The relative amount of transition metal catalyst can be decreased. The amount of undesired byproduct is also reduced.
Abstract:
Novel aromatic polycyclic retinoid-type derivatives of general formula (I), wherein groupings R3 and R4 attached to the double bond between carbons 11 and 12 are cis groupings, and pharmaceutical and cosmetic compositions containing same, are disclosed.
Abstract:
A compound of formula (I), wherein R and R are independently selected from chloro, fluoro, bromo, C1-6 alkyl, C1-6 alkoxy or C1-6 haloalkyl provided that both R and R are not fluoro; R and R are independently selected from hydrogen and C1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.
Abstract translation:式(I)化合物,其中R 1和R 2独立地选自氯,氟,溴,C 1-6烷基,C 1-6烷氧基或C 1-6卤代烷基,条件是R 1和 R 2不是氟; R 3和R 4独立地选自氢和C 1-6烷基,及其药学上可接受的盐,溶剂合物或生理功能衍生物,它们在药物中的用途,特别是肺炎或治疗与炎症,关节炎, 或疼痛,包含它们的药物组合物及其制备方法。
Abstract:
Novel 3,4-dihydro-4-oxo-3-(prop-2-enyl)-1-phtalazineacetic acids and derivatives of formula (I) in which R1, R2 and R3 are the same or different and stand for H, a halogen or a linear or branched aliphatic, saturated or unsaturated radical, substituted or not by at least one halogen or R4 residue such as defined below, except when R4 is H; R4 and R5 are the same or different and stand for H, a linear or branched aliphatic radical, saturated or unsaturated, an aryl or heteroaryl radical, said radicals being substituted or not by at least one grouping such as fluorine, chlorine, bromine, methyl or trifluoromethyl, where R4 and R5 do not simultaneously denote H; R6 stands for a hydroxy or alkoxy radical; R7 stands for H, a halogen, a linear or branched aliphatic saturated or unsaturated radical, an alkoxy radical, said radicals being substituted or not by an aliphatic or halogenated radical, a nitro group, a substituted or unsubstituted amino group, S(O)n R8 or a cyano group; n is equal to 0, 1 or 2; R8 is an aliphatic, linear or branched radical, an aryl or heteroaryl radical, an amino radical, said radicals being substituted or not by an aliphatic or halogenated radical. The invention also relates to the optional tautomeric forms of said acids and their pharmaceutically acceptable base addition salts. Also described is a process for preparing said compounds and the drugs containing same.
Abstract:
本发明涉及塔式连续光氯化法制氯苄,使化学式为(X) a C 6 H 6-a-b (CH 3 ) b 的芳烃类化合物在流动中成液膜,与氯气在光照条件下进行膜界面光氯化反应,反应开始时侧链甲基上的一个氢被氯取代生成一氯苄。并可以继续通入氯气反应,苄基上的两个氢被氯取代生成二氯苄,以此类推,侧链甲基上的氢逐渐被氯取代,并最终可以得到侧链甲基上的氢全部被氯取代的产物。本申请的主要优点在于:副反应少,产品收率高,产品纯度高,且易于进一步纯化,反应效率高,生产时间短,适宜于工业化生产。
Abstract:
This invention relates to fluorinating agents and, more particularly, to chiral non-racemic fluorinating agents useful for enantioselective fluorination, as well as to their synthesis and use and other subject matter. The fluorinating agents are based on a substituted 1,4-diazabicyclo[2.2.2]octane (DABCO) skeleton and provide electrophillic fluorine enantioselectively.