摘要:
The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkanoic and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.
摘要:
A process provided for the production of 2-nitrobenzaldehyde from 2-nitrotoluene, in which 2-nitrotoluene is converted, by bromination by a radical mechanism, to 2-nitrobenzyl bromide in the form of a bromination oil containing 20 to 50% or more of 2-nitrobenzyl bromide, and the bromination oil is oxidized directly with a mixture of dimethylsulphoxide and sodium bicarbonate in a weight ratio of 3:1 to 10:1 at temperatures of up to 100.degree. C. and the 2-nitrobenzaldehyde is subsequently isolated via the bisulphite adduct, to give 2-nitrobenzaldehyde in high purity and high yield. The process also has the advantage of a very short reaction time. The 2-nitrobenzaldehyde produced is an important intermediate, for example in the production of pharmaceutically active 1,4-dihydropyridines.
摘要:
A benzylalcohol derivative of the formula: ##STR1## wherein R is hydroxy, benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is monomethoxyphenyl, dimethoxyphenyl, trimethoxyphenyl or 3,4-methylenedioxyphenyl is prepared by reducing a compound of the formula: ##STR2## wherein R' is benzyloxy, alkoxy of one to 4 carbon atoms or halogen, and Ring A is the same as defined above, and when R' is benzyloxy, if required, further subjecting the product to catalytic hydrogenation.The compounds (I) and pharmaceutically acceptable acid addition salts thereof are used as anti-diabetic agents.
摘要:
The present invention relates to a process for the preparation of 4,4'-difluorobenzophenone. 4,4-difluorobenzophenone may be prepared by diazotization of 4,4'-diamino-diphenylmethane in anhydrous or concentrated aqueous hydrogen fluoride, decomposition of the diazonium fluoride thus produced to yield 4,4'-difluoro-diphenylmethane and oxidation of 4,4'-difluoro-diphenylmethane to yield 4,4'-difluorobenzophonone.Thus, according to the present invention, there is provided a process for the preparation of 4,4'-difluorobenzophenone which comprises the following steps:(1) diazotization of 4,4'-diamino-diphenylmethane in anhydrous or concentrated aqueous hydrogen fluoride to yield a solution of a corresponding diazonium fluoride; and(2) (i) thermally decomposing the diazonium fluoride in the solution thus produced to yield 4,4'-difluoro-diphenylmethane and (ii) subsequently oxidizing the 4,4'-difluoro-diphenylmethane to yield 4,4'-difluorobenzophenone.
摘要:
A method for preparing aromatic aldehydes and ketones in which the aldehydo or keto group is bonded directly to the aromatic ring; which comprises oxidizing an alkyl substituted aromatic compound or an aromatic compound which is substituted by an alpha-hydroxyalkyl moiety, via treatment with a persulfate and a metal catalyst. The metal catalysts include, for example, (1) iron salts and silver salts, or (2) a redox pair of salts such as an iron salt in combination with a copper salt or a silver salt in combination with a copper salt.
摘要:
A compound of the formula: ##STR1## wherein R is lower alkyl, may be prepared, for example, by reducing a compound of the formula: ##STR2## wherein R is same as above. Other methods for preparing the compound [I] are also disclosed. The compound [I] and a pharmaceutically acceptable acid addition salt thereof are useful as anti-diabetic agents.
摘要:
Compounds possessing hypoglycemic, hypotensive, anti-inflammatory, anticoagulant and diuretic activity are represented by compounds of the following formula ##STR1## where Y is thienyl, cycloalkyl of from 5 to 7 carbon atoms, phenyl or substituted phenyl in which case the substituents on the substituted phenyl are selected from halogen, such as fluorine, chlorine, bromine or iodine, lower alkyl of from 1 to 4 carbon atoms and lower alkoxy of from 1 to 4 carbon atoms; Z is hydrogen or hydroxy; R is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl of from 1 to 4 carbon atoms or halogen, such as chlorine, fluorine, bromine or iodine; m is from 3 to 6; and n is from 3 to 11. Pharmaceutical compositions of these compounds and their use are also disclosed.
摘要:
A method for the homogeneous catalytic enantioselective hydrogenation of alkyl and alkenyl substituted acrylic acids wherein these acids are selectively hydrogenated at the double bond alpha,beta to the acid function, said hydrogenations are catalyzed by rhodium complexes of chiral tertiary phosphines. This method provides a route to chiral dihydrogeranic acid and other intermediates useful in the synthesis of chiral vitamin E, citronellal, and menthol. Novel chiral tertiary phosphines are also disclosed.
摘要:
New fluoro derivatives of aralkylamine compounds, particularly 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine, as well as the N-alkyl and the N,N-dialkyl derivatives thereof are prepared by reaction of 2-bromobenzonitrile with benzylmagnesium chloride to produce 2'-bromo-2-phenylacetophenone; oxidation of said acetophenone with selenous acid to produce 2-bromobenzil; conversion of the benzil compound by treatment with sulfur tetrafluoride to the corresponding 2-bromo-.alpha.,.alpha.-.alpha.',.alpha.'-tetrafluorobibenzyl;followed by reaction of the 2-bromobibenzyl compound with a metal cyanide to produce the corresponding 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzonitrile. This nitrile compound is then reduced with lithium aluminum hydride to produce the corresponding benzylamine, which is then converted, if desired, to the N-alkyl and/or N,N-dialkyl 2-(2-phenyl-1,1,2,2-tetrafluoroethyl)benzylamine. Alternatively, the nitrile or the precursor bromobibenzyl can be converted by Grignard reactions to the corresponding .alpha.-alkyl or .alpha.,.alpha.-dialkylbenzylamine which can then be converted if desired to the corresponding N-alkyl and/or N,N-dialkyl substituted benzylamine compound. The phenyltetrafluoroethylbenzylamine as well as its N-alkyl and N,N-dialkyl derivatives are active as antiarrhythmic agents.
摘要:
Process for improving, enhancing or modifying the organoleptic properties of a tobacco product, which comprises adding thereto about 1 to about 1000 parts per million based on the weight of tobacco of octa-3,5-dien-2-one.