专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-2009131688-A1 优先权日:2007-11-21 标 题 :Method for the synthesis of 4-benzofuran-carboxylic acid 发明人:BURGOS ALAIN; MARUANI MARTINE; PERRIN FLORENCE; FREIN STEPHANE 权利人:ZACH SYSTEM 摘要:The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. n This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: n n n n n n n n n n wherein R independently represents hydrogen or a linear or branched C 1 - 15 alkyl group. n With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.
专利号:US-6524446-B2 优先权日:2001-03-27 标 题 :Process for synthesis of a porphyrin compound using a molecular sieve catalyst under microwave irradiation 发明人:KULKARNI SHIVANAND JANARDAN; RAGHAVAN KONDAPURAM VIJAYA; MOTKURI RADHA KISHAN; NAGABANDI SRINIVAS 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides an improved process for synthesis of porphyrin compounds of the general formula 1 n from pyrrole and aromatic aldehyde over zeolite molecular sieve catalysts using microwave heating, (solvent free) to provide an eco-friendly, economical, faster and selective heterogeneous method.
专利号:US-5679864-A 优先权日:1995-11-03 标题:Process for the synthesis of curcumin-related compounds 发明人:KRACKOV MARK HARRY; BELLIS HAROLD EDWARD 权利人:GENE PRINT INC 摘要:The invention is directed to a process for the synthesis of curcumin and curcumin-related compounds by reacting the enol form of a 2,4-diketone with a monocarbocyclic aldehyde in the presence of an organic amine catalyst. The reactants are dissolved in a highly polar, aprotic organic solvent. The curcumin-related product is recovered in crystalline form by precipitation from the reaction mass and solvent recrystallization.
专利号:US-5763681-A 优先权日:1989-09-06 标 题 :Synthesis of stable, water-soluble chemiluminescent 1,2-dioxetanes and intermediates therefor 发明人:EDWARDS BROOKS; JUO RHOU-RONG 权利人:TROPIX INC 摘要:A novel synthesis of compound having the formula: ##STR1## wherein T is a stabilizing spiro-linked polycycloalkylidene group, R 3 is a C 1 -C 20 alkyl, aralkyl or heteroatom containing group, Y is an aromatic fluorescent chromophore, and Z is a cleavable group which, when cleaved, induces decomposition of the dioxetane ring and emission of optically detectable light, is disclosed. A tertiary phosphorous acid alkyl ester of the formula: n n (R.sup.1 O).sub.3 P n n wherein R 1 is a lower alkyl group, is reacted with an aryl dialkyl acetal produced by reacting a corresponding aryl aldehyde with an alcohol of the formula: n n R.sup.3 OH n n wherein R 3 is as defined above, to produce a 1-alkoxy-1-aryl-methane phosphonate ester of the formula: ##STR2## reacting the phosphonate with base to produce a phosphonate-stabilized carbanion, reacting the carbanion with a ketone of the formula: ##STR3## wherein T is as defined above, to produce an enol ether of the formula: ##STR4## then oxygenating the double bond in the enol ether to give the corresponding 1,2-dioxetane compound.
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合成参考文献
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