| 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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