专利号:US-5827794-A 优先权日:1994-02-22 标 题 :Supported highly-polar liquid phase chiral sulfonated binap catalyst for asymmetric synthesis of optically active compounds 发明人:DAVIS MARK E; WAN KAM TO 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention relates to water soluble chiral sulfonated 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl and its use as organometallic catalysts for asymmetric synthesis of optically active compounds. Asymmetric reactions of the present invention include those reactions in which organometallic catalysts are commonly used. Such reactions include, but are not limited to, reduction and isomerization reactions on unsaturated substrates and carbon--carbon bond forming reactions. Examples of such reactions include, but are not limited to, hydrogenation, hydroboration, hydrosilylation, hydride reduction, hydroformylation, alkylation, allylic alkylation, arylation, alkenylation, epoxidation, hydrocyanation, disilylation, cyclization and isomerization reactions. n The catalysts of the present invention provide the advantage of functioning in the presence of water without loss in enantioselectivity relative to the nonsulfonated BINAP catalyst in an organic solvent. As a result, the catalysts of the present invention may be employed in water, water miscible solvents, in aqueous--organic two phase solvent systems and in supported aqueous phase catalysts in organic solvents without loss in enantioselectivity. Further, the catalysts of the present invention may also be effectively employed in highly polar solvents such as primary alcohols and ethylene glycol. n The present invention also relates to a method for conducting asymmetric reactions on prochiral unsaturated bonds contained within a compound using the water soluble chiral sulfonated 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl organometallic catalysts of the present invention.
专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-5688968-A 优先权日:1993-03-22 标题 :Enantioselective synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno 2,3-B!thiopyran-2-sulfonamide 7,7-dioxide 发明人:BLACKLOCK THOMAS J; MATHRE DAVID J; SOHAR PAUL 权利人:MERCK & CO INC 摘要:A key step in the synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide (dorzolamide) and related compounds is a Ritter reaction with an unexpected tendency to proceed with retention of chirality.
专利号:US-11459427-B1 优先权日:2021-10-07 标题 :Synthesis of polyaniline or derivatives thereof 发明人:ALAMRY KHALID A; KHAN AJAHAR; ASIRI ABDULLAH MOHAMED 权利人:UNIV KING ABDULAZIZ 摘要:Provided are synthesis methods of polymerizing aniline or derivatives thereof. The production of polyaniline or polyaniline derivatives is controlled by the type of oxidant added in the reaction medium. The methods include the step of using a safe and environmentally friendly carbomethyl cellulose (CMC) or modified CMC as an oxidant in the polymerization reaction to produce polyaniline or aniline derivatives. Synthesis methods of producing O-CMC and O-CMC-S oxidants are also provided herein.
专利号:US-4374979-A 优先权日:1981-04-27 标 题:Regiospecific synthesis of anthracyclinone compounds such as daunomycinone 发明人:MITSCHER LESTER A 权利人:UNIV KANSAS ENDOWMENT ASS 摘要:A regiospecific synthesis for anthracyclinones asymmetric is disclosed. The synthesis is based upon a regiospecific bromination of the C-7 position of the alpha -tetralone which after transposing the keto group to the beta -position and reaction with an organo-lithium compound is condensed with a phthalate ester.
专利号:US-5189206-A 优先权日:1989-03-16 标题 :Process for the preparation of aminobenzenesulfonic acids 发明人:HERZIG PAUL 权利人:CIBA GEIGY CORP 摘要:There is disclosed a process for the preparation of compounds of formula ##STR1## wherein the symbols are as defined in claim 1, which process comprises dissolving a compound of formula ##STR2## in sulfuric acid, adding this solution to oleum and reacting the mixture in the temperature range from 10° to 80° C. until a sulfo group has been completely introduced, and, in an optional further step, subjecting the reaction mixture to further reaction in the temperature range from 100° to 200° C. to introduce a second sulfo group. n The compounds of formula (1) obtainable by this process are useful intermediates for the synthesis of dyes and are particularly suitable diazo components for the synthesis of azo dyes.