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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
441 Strong base reagent US454455 1989-12-21 US5078906A 1992-01-07 Kuen-Wai Chiu; Mary H. Staruch; David H. Ellenberger
.alpha.-Arylalkanoic acids are prepared by a method comprising the step of reacting an alkylaromatic compound corresponding to the desired .alpha.-arylalkanoic acid with a new metallation reagent solution. The reagent comprises the reaction product of alkyllithium or aryllithium and about two to five molar equivalents of potassium tert-alkoxide in a trialkylamine solvent.
442 Preparation of 3-vinyl-substituted 2,2-dimethylcyclopropane-1-carboxylic acids and esters and intermediates therefor US355578 1989-05-22 US4992577A 1991-02-12 Reinhard Lantzsch; Dieter Arlt; Manfred Jautelat
A process for preparing a compound of the formula ##STR1## in which Y is halogen, alkyl or cycloalkyl optionally substituted by halogen or C.sub.1-4 -alkoxy, alkenyl optionally substituted by halogen, aryl, heteroaryl or alkoxycarbonyl,X is hydrogen, halogen or optionally halogen-substituted alkyl, orX and Y, together with the adjacent C atom, form a saturated cycloalkphatic ring having up to 6 C atoms, andR is hydrogen or C.sub.1 -C.sub.4 -alkyl, comprising reacting an aldehyde of the formula ##STR2## with 2-methylbutan-3-one of the formula ##STR3## in the presence of a hydrohalic acid thereby to form a 4,4-dimethyl-3-halogeno-1-hexen-5-one of the formula ##STR4## in which Hal is halogen, halogenating said compound to produce a compound of the formula ##STR5## and reacting said compound with a base of the formulaR--OM (VI)in whichM is one equivalent of an alkali or alkaline earth metal ion.Compounds IV and V are new. By suitable conditions the trans isomer is selectively produced.
443 Process for the preparation of trans-2,2-dimethyl-3-(2,2-dichlorovinyl)-cyclopropanecarboxylic acid US422840 1989-10-17 US4987251A 1991-01-22 Reinhard Lantzsch; Karl Steinbeck
A process for the preparation of trans-2,2-di-methyl-3-(2,2-dichlorovinyl)-cyclopropanecarboxylic acid of the formula (I) ##STR1## comprising reacting a chloroketone of the formula (II) ##STR2## in which Z represents chlorine or bromine,with an aqueous solution of an alkali metal hydroxide.
444 Stereoconvergent process for preparing optically active carboxylic acids US137000 1987-12-23 US4922009A 1990-05-01 Marco Villa; Claudio Giordano; Graziano Castaldi; Silvia Cavicchioli
A stereoconvergent process is described for preparing optically active alpha-arylalkanoic acids using as starting substance a diastereoisomeric mixture of ketals of formula ##STR1## in which the substituents have the meanings given in the description. The described process leads to the formation of a single enantiomer.
445 Process for the preparation of 3-(2-chloro-2-(4-chloro-phenyl)-vinyl)-2,2-dimethylcyclopropanecarboxyli c acid US290216 1988-12-27 US4897505A 1990-01-30 Reinhard Lantzsch
3-(2-chloro-2-(4-chloro-phenyl)-vinyl)2,2-dimethylcyclopropanecarboxylic acid and its derivatives are obtained by reactive 3-chloro-3(4-chlorophenyl)-propenal with chloromethyl isopropyl ketone in a first step and reacting the resulting 4,4-dimethyl-1,3,6-trichloro-1-(4-chlorophenyl)- hex-1-en-5-one, optionally without isolation, in the presence of aqueous bases or in the presence of alkoxides. The resulting carboxylic acids or carboxylic acid esters can be converted into their derivatives such as, for example, salts, esters, amides or halides by generally known methods.
446 Process for the preparation of optically active alpha-arylalkanoic acids and novel intermediates thereof US82196 1987-08-05 US4888433A 1989-12-19 Claudio Giordano; Graziano Castaldi; Fulvio Uggeri; Silvia Cavicchioli
A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration. This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions. The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids.
447 Intermediates for preparing optically active carboxylic acids US891349 1986-07-31 US4861903A 1989-08-29 Claudio Giordano; Graziano Castaldi
A process is described for preparing optically active alpha-arylalkanoic acids consisting of rearranging an optically active ketal of formula ##STR1## in which the substituents have the meaning given in the description of the invention.
448 Method for producing cyclopropanecarboxylic acid derivatives US82942 1987-08-07 US4772753A 1988-09-20 Noritada Matsuo; Kazunori Tsushima
A method for producing 2,2,3,3-tetramethylcyclopropane-1-carboxylic acid and intermediate compounds thereof. The 2,2,3,3-tetramethylcyclopropane-1-carboxylic acid is a very useful intermediate for synthesizing insecticidal and acaricidal compounds of pyrethroid type.
449 Process for preparing naproxen US732735 1985-05-10 US4736061A 1988-04-05 Oreste Piccolo; Ermanno Valoti; Giuseppina Visentin
Process for preparing Naproxen via a sequence of stereospecific reactions which comprises: condensation of 1-chloro-2-methoxy-naphthalene with a (S)-2-halo-propionyl halide according to the Friedel-Crafts reaction, ketalization of the thus obtained (S)-2-halo-1-(5'-chloro-6'-methoxy-2'-naphthyl)-propan-1-one, rearrangement of said ketal to afford an ester, hydrolysis of the ester and removal of the chlorine atom in 5-position by hydrogenolysis.New (S) 2-halo-1-(5'-chloro-6'-methoxy-2'-naphthyl)-propan-1-ones.
450 Process for the preparation of pyrethroid acids US871153 1986-05-30 US4691052A 1987-09-01 William T. Brady; Scott J. Norton; Jinrea Ko
Pyrethroid acids are prepared by conducting a cycloaddition reaction of a conjugated diene and a dihaloketene to form a dihalo-vinylcyclobutanone product; reducing the dihalo-vinylcyclobutanone product to a monohalo-vinylcyclobutanone product and then conducting a ring contraction with a base to form the desired acid product.
451 Method for preparing (+)S-2--hydroxy-2-methyl-hexanoic acid US894390 1986-08-11 US4668822A 1987-05-26 Paul F. Corey
A method for preparing an important stereo-specific intermediate in the synthesis of prostaglandin analogs is disclosed. Said intermediate is (+)S-2-hydroxy-2-methyl-hexanoic acid and is prepared via an asymmetric halolactonization reaction utilizing L-proline as the chiral agent.
452 Preparation of 2,2-dimethyl-3-aryl-cyclopropanecarboxylic acid and esters and new intermediates therefor US805502 1985-12-04 US4663465A 1987-05-05 Reinhard Lantzsch; Dieter Arlt; Manfred Jautelat
2,2-Dimethyl-3-arylcyclopropanecarboxylic acids and esters, suitable as insecticide intermediates, of the formula ##STR1## in which Ar is naphthyl or substituted furyl, thienyl or phenyl, andR.sup.1 is hydrogen or alkyl, are produced by subjecting ##STR2## to radical polymerization to produce ##STR3## reacting that with chlorine or bromine to produce ##STR4## and reacting that with an alkali metal or alkaline earth metal hydroxide or carbonate. Various intermediates II and III are new.
453 Method for manufacture of 7-(2,5-dioxocyclopentyl)heptanoic acid derivative US695187 1985-01-28 US4658055A 1987-04-14 Takashi Onuki; Hirokazu Naora; Asao Nakamura
A method for the manufacture of a heptanoic acid derivative represented by the formula ##STR1## wherein R.sup.3 stands for an acyloxy group, a halogen atom, or a hydrogen atom, which comprises reacting a cyclooctene derivative represented by the formula ##STR2## wherein Y stands for --R.sup.1, --COR.sup.1 or --SiR.sup.2.sub.3, wherein R.sup.1 is an alkyl group, an aryl group, or an aralkyl group and R.sup.2 is an alkyl group of 1 to 5 carbon atoms, with a compound represented by the formula ##STR3## wherein R.sup.3 has the same meaning as indicated above and X.sup.1 and X.sup.2 each is a halogen atom, is described along with uses for such compounds.
454 Process for producing an .alpha.-aromatic group substituted alkanoic acid derivative US722833 1985-04-12 US4649213A 1987-03-10 Takayoshi Yamauchi; Kaneaki Hattori; Shun-ichi Ikeda; Kenji Nakao; Kentaro Tamaki
Compounds having anti-inflammatory and analgesic activity of the formula ##STR1## are produced from compounds having the formula ##STR2## by rearrangement in the presence of a base or an amide and (1) X S O X.sup.1 or X S O.sub.2 X.sup.1 where X and X.sup.1 are halogen or trifluoromethyl or (2) sulfur dioxide and halogen.
455 Therapeutically useful pseudopeptides, compositions containing the same and methods of preparation and use US715424 1985-03-25 US4631270A 1986-12-23 John A. Yankeelov, Jr.; Kam-Fook Fok
Therapeutically useful pseudopeptides characterized by the replacement of at least one peptide group, both in a naturally occurring peptide or protein by a thiomethylene group are useful in the treatment of various metabolic malfunctions.
456 Process for the preparation of arylalkanoic acids by oxidative rearrangement of arylalkanones US754538 1985-07-12 US4608441A 1986-08-26 Attilio Citterio; Laura Tinucci; Aldo Belli; Lucio Filippini
Process for preparing an arylalkanoic acid by adding iodine to a mixture of an arylalkanone and an excess of an orthoester, heating of the mixture thus obtained, adding an inorganic base and finally an acid.
457 Process for the preparation of optically active alpha-arylalkanoic acids US704406 1985-02-22 US4579968A 1986-04-01 Graziano Castaldi; Claudio Giordano; Fulvio Uggeri
A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active (alpha-haloalkyl)-aryl-ketals and in submitting to hydrolysis the thus obtained esters of alpha-arylalkanoic acids. The rearrangement reaction is carried out under neutral or alightly alkaline conditions, in an aprotic dipolar diluent and in the presence of a protic substance having a high dielectric constant.
458 Biaryl aldehyde US650981 1984-09-14 US4578522A 1986-03-25 John F. Eaddy, III
This invention relates to a method of synthesis of certain substituted carboxylic acids useful in lowering serum triglyceride and total cholesterol levels in mammals (including man) represented by the general formula I:Ar.sup.1 --Ar.sup.2 (I)whereinAr.sup.1 is selected from ##STR1## Ar.sup.2 is selected from ##STR2## and R is selected from C.sub.1-5 alkyl, halogen, perhalo-C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl, C.sub.1-4 acyl, C.sub.1-6 alkoxycarbonyl, amino or hydroxy.
459 Process for the preparation of fluorene-9-carboxylic acid US552459 1983-11-16 US4564700A 1986-01-14 Winfried Orth; Emmerich Pastorek; Werner Fickert
An improved process for the preparation of fluorene-9-carboxylic acid comprising reacting fluorene and a dialkyl carbonate with alkyls of 1 to 5 carbon atoms in the presence of a member of the group consisting of alkali metal hydrides or potassium alcoholate of an aliphatic alcohol of 1 to 5 carbon atoms, neutralizing the mixture and saponifying the resulting fluorene-9-carboxylic acid ester to obtain fluorene-9-carboxylic acid in good yields.
460 Mobile atom insertion reaction, mobile atom transmissive membrane for carrying out the reaction, and reactor incorporating the mobile atom transmissive membrane US618014 1984-06-07 US4547273A 1985-10-15 William Ayers
Disclosed is a method of carrying out a mobile atom insertion reaction, such as a hydrogen insertion reaction, for the synthesis of reduced, hydrogenated compounds. Such reactions include the production of ammonia and hydrazine from nitrogen, formic acid and methanol from carbon dioxide, and hydrogen peroxide from oxygen. The insertion reactions are carried out at a bipolar mobile atom transmissive membrane comprising a membrane formed of a mobile atom pump material, as a hydrogen pump material, conductive atom transmissive means on one surface of the membrane and conductive atom transmissive means on the opposite surface of the membrane. The mobile atom, such as hydrogen, diffuses across the membrane, to provide a source of hydrogen on the insertion reaction side of the membrane. The insertion reaction side of the membrane is positively biased with respect to a counterelectrode so that a reactant molecule, such as carbon dioxide, is electrosorbed on that surface of the membrane. The electrosorbed reactant molecule chemically reacts with the surface hydrogen by the insertion reaction to form a reduced, hydrogenated product such as formic acid. Also disclosed is a chemical reactor, containing the membrane, and several electric field assisted chemical reactions utilizing the membrane and reactor.
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