专利号:US-6590119-B2 优先权日:1999-06-11 标题 :Methods for the synthesis of dioxoalkanoic acid compounds 发明人:FERRO MICHAEL P; MCCOY KATHLEEN A 权利人:ORTHO MCNEIL PHARM INC 摘要:The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.
专利号:WO-2023035571-A1 优先权日:2021-09-10 标 题:Synthesis method for esaxerenone and intermediate thereof 发明人:RUAN JING; ZHANG XINXIN; YAN GONGCHAO; RUAN XIAONA; ZHANG WEI 权利人:SHANGHAI DINGYA PHARMACEUTICAL CHEMICALS CO LTD 摘要:Provided is a new synthesis method for an intermediate of esaxerenone. The method comprises: (1) reacting 2-(trifluoromethyl)phenylacetic acid as a raw material with ethyl chloroformate or isobutyl chloroformate in an inert solvent in the presence of an alkali to produce a mixed anhydride, then reacting same with ammonia to obtain a corresponding amide compound of formula II; (2) subjecting the amide compound of formula II obtained in step (1) to a dehydration reaction in the presence of a dehydrating agent and an acid-binding agent to obtain an isocyanide compound of formula III; and (3) subjecting the isocyanide compound of formula III obtained in step (2) to a cyclization reaction with ethyl 2-butynonate in the presence of an alkali and a metal catalyst to form a pyrrole ring compound of formula IV; and the reaction equation is shown below: Compared to the prior art, the technical solution of the present invention has the advantages of a high yield, a simple post-treatment, low costs and easy industrialization, etc.
专利号:US-4719053-A 优先权日:1980-08-01 标题 :Beta-chloroethylsulfonylmethyl-benzoic halides as intermediates 发明人:SCHLAEFER LUDWIG; HAEHNLE REINHARD 权利人:HOECHST AG 摘要:New beta -chloroethylsuflonylmethyl-benzoic acid halides which can serve as fibre-reactive anchors for thesynthesis of novel organic, water-soluble compounds, preferably dyestuffs, having fibre-reactive and fibre-finishing properties, such as preferably dyestuff properties, and containing, as a fibre-reactive group, one or two beta -chloroethylsufonylmethylbenzoic acid amide groups. For the synthesis of these novel fibre-finishing compounds, said new beta -chloroethylsulfonylmethyl-benzoic acid halide compounds are reacted with an organic, water-soluble compound having fibre-finishing properties and continuing one or two amino groups. Also precursors of the fibre-finishing, fibre-reactive compounds, containing said beta -chloroethylsulfonylmethyl-benzxoic acid amid grouping, can be employed for their synthesis. The novel fibre-finishing compounds can be applied onto suitable fibre materials, such as especially cellulose fibre material and natural or synthetic polyamide fibre materials, and fixed on these fibre materials in a manner similar to application and fixation methods usual in the technique for fibre-reactive compounds. The fibre-finished material, such as dyed material, shows very good wet fastnesses.
专利号:US-2007060558-A1 优先权日:2004-07-30 标 题 :Hybrid molecules QA where Q is an aminoquinoline and A is an antibiotic residue, the synthesis and uses thereof as antibacterial agents 发明人:SANCHEZ MURIEL; MEUNIER BERNARD 权利人:CENTRE NAT RECH SCIENT 摘要:The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q—(Y 1 ) p —(U) p —(Y 2 ) p -A: wherein Q represents an aminoquinoline, (Y 1 ) p (U) p —(Y 2 ) p″ is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.
专利号:US-4257942-A 优先权日:1977-10-06 标题:New water-insoluble azo dyes 发明人:DEFEO FRANCESCO; CIPOLLI ROBERTO 权利人:ACNA 摘要:The present invention relates to the synthesis of new dyes having the following general formula: wherein: D is the residue of a diazotizable component of the carbocyclic or heterocyclic series X is an ethylene group, optionally substituted by halogen-methyl, alkyl C1-C4, aryl, aralkyl or CH2OCO(HN)nR (wherein R and n have the meanings hereinafter defined); R is alkyl C1-C8 optionally substituted by halogen, CN,COOH; aryl optionally substituted by one or more atoms of halogen, alkyl C1-C4, alkoxyl C1-C4; alkoxyl C1-C4; alkoxyl C1-C8; Aryloxy; aralkoxy; cycloalkoxy; aralkyl; naphthyl optionally substituted by halogen; alkenyl C2-C8, optionally substituted by halogen, CN, COOH; R1 and R2, either like or unlike each other, may be alkyl C1-C4 optionally substituted by halogen or CN groups; aralkyl; R3 is H; halogen, alkyl C1-C4; alkoxyl C1-C4, optionally substituted. n is 0 or 1.
专利号:US-4740604-A 优先权日:1986-05-26 标题:Benzanthrone lactones 发明人:WEIS CLAUS D; SUTTER PETER 权利人:CIBA GEIGY CORP 摘要:There are disclosed benzanthrone lactones of formula ##STR1## wherein R 1 , R 2 and R 3 are as defined in claim 1. The benzanthrone lactones of formula (1) are important intermediates for the synthesis of novel dyes which are obtained by coupling suitable diazo components to said compounds of formula (1).
摘要:Tong, M. L.; Kunz, K.; Jaschinski, M.; Holzschneider, K.; Celik, I. E.; Kirsch, S. F., Science of Synthesis Knowledge Updates, (2020) 2, 259. 摘要:F. G. Bordwell and G. D. Cooper. J. Am. Chen. Soc. 74, 1058 (1952). 摘要:S. Shanmuganathan and N. Vanajakshi. J. Indian Chem. Soc. 46, 79 (1969). 摘要:K.B. Whetsel. Spectrochim. Acta 17, 617 (1961). 摘要:Solorio-Alvarado, C. R., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .