3-溴-4-氟苯甲醇置于potassium Dichromate,硫酸体系中,用 二氯甲烷,水 作为反应溶剂,化学反应生成 3-溴-4-氟苯甲醛 参考文献:Preparation Of 4-Fluoro-3-Phenoxy-Benzal-Dehyde Acetals And 标题:Preparation Of 4-Fluoro-3-Phenoxy-Benzal-Dehyde Acetals And 摘要:新化合物##str1##被制备并转化为新的缩醛##str2##,然后在存在铜或铜化合物作为催化剂和稀释剂的情况下,在约100度至200度c的温度下,与碱性酚酚盐或碱土金属酚酚盐发生反应,反应生成新的缩醛##str3##,可以水解成相应的醛,这是拟除虫剂的已知中间体.
专利号:US-4383949-A 优先权日:1980-07-16 标题:Preparation of 3-bromo-4-fluorobenzaldehyde and its acetals 发明人:MAURER FRITZ; RIEBEL HANS-JOCHEM; PRIESNITZ UWE; KLAUKE ERICH 权利人:BAYER AG 摘要:A process for the preparation of a 3-bromo-4-fluorobenzaldehyde acetal of the formula ##STR1## in which R 1 is methyl or ethyl, n which comprises reacting a 3-bromo-4-fluoro-benzoic acid halide with ammonia to form 3-bromo-4-fluoro-benzoic acid amide, dehydrating said amide to form 3-bromo-4-fluoro-benzonitrile, reacting the nitrile with formic acid in the presence of a catalyst at a temperature between about 0° and 150° C. to form 3-bromo-4-fluorobenzaldehyde, and reacting said aldehyde with R 1 OH or a derivative thereof capable of forming an acetal. The amide and nitrile are new compounds. The acetals are known intermediates in the synthesis of pyrethroid-like insecticides.
专利号:US-2021284618-A1 优先权日:2016-08-12 标 题 :Furanochalcones as inhibitors of cyp1a1, cyp1a2 and cyp1b1 for cancer chemoprevention 发明人:BHARATE SANDIP BIBISHAN; SHARMA RAJNI; JOSHI PRASHANT; VISHWAKARMA RAM; CHAUDHURI BHABATOSH 权利人:COUNCIL SCIENT IND RES; DE MONTFORT UNIV 摘要:The present invention relates to the furanochalcone class of compounds of general formula A. The present invention particularly relates to the synthesis of furanochalcones and their CYP1A1, CYP1A2 and CYP1B1 inhibitory activity. In addition, the invention relates to the prevention or treatment of cancer caused by polyaromatic hydrocarbons (PAHs), 4-nitroquinoline-1-oxide, and N-nitroso-N-methylurea, heterocyclic amines, estrogen and 17β-estradiol, resulting from the inhibition of CYP1A1, CYP1A2 and CYP1B1 enzymes.
专利号:US-8273793-B2 优先权日:2007-12-07 标题:Method for producing precursors for L-2- [18F] fluorophenylalanine and 6- [18F] fluoro-L—meta-tyrosine and the α-methylated derivatives thereof, precursor, and method for producing L-2- [18F] fluorophenylalanine and 6- [18F] fluoro-L-meta-tyrosine and the α-methylated derivatives from the precursor 发明人:WAGNER FRANZISKA; ERMERT JOHANNES; COENEN HEINRICH HUBERT 权利人:WAGNER FRANZISKA; ERMERT JOHANNES; COENEN HEINRICH HUBERT; FORSCHUNGSZENTRUM JUELICH GMBH 摘要:Disclosed is a method for producing precursors for 2-[ 18 F]fluorophenylalanine and 6-[ 18 F]fluoro-L-meta-tyrosine and the α-methylated derivatives thereof, to the precursor, and to a method for producing 2-[ 18 F]fluorophenylalanine and 6-[ 18 F]fluoro-L-meta-tyrosine and the α-methylated derivatives thereof from particular precursor. A compound of formula (3) is provided which enables an automated synthesis of L-3,4-dihydroxy-6-[ 18 F]fluorophenylalanine and 6-[ 18 F]fluoro-L-meta-tyrosine. The enantiomeric purity of the product is ≧98%.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-4446075-A 优先权日:1980-02-22 标 题:Substituted bromofluorobenzene derivatives and process for its manufacture 发明人:EIGLMEIER KURT; KNIEPS REINHARD 权利人:RIEDEL DE HAEN AG 摘要:Substituted bromofluorobenzene, wherein the fluorine is in para-position and the bromine in meta-position to another substituent, is prepared by direct bromination of the corresponding fluorobenzene derivative. Bromination is advantageously carried out in the presence of a catalyst, preferably a metal or metal salt. The elementary bromine is used in an amount of 0.9 to 1.3 mols per mol of fluorobenzene derivative and the reaction temperature is between 20° and 200° C. The bromofluorobenzene derivatives are suitable for the synthesis of medicaments and plant protective agents.
专利号:US-12227528-B2 优先权日:2017-11-09 标 题:Glucose-sensitive albumin-binding derivatives 发明人:KRUSE THOMAS; KOFOD-HANSEN MIKAEL; MUENZEL MARTIN WERNER BORCHSENIUS; THOEGERSEN HENNING; SAUERBERG PER; EWALD JAKOB; BEHRENS CARSTEN; HOEG-JENSEN THOMAS; BALSANEK VOJTECH; DROBNAKOVA ZUZANA; DROZ LADISLAV; HAVRANEK MIROSLAV; KOTEK VLADISLAV; STENGL MILAN; SNAJDR IVAN; DRUSANOVA HANA 权利人:NOVO NORDISK AS 摘要:This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates.
[参考文献]: Guomin Shan, Et Al. A Sensitive Class Specific Immunoassay For The Detection Of Pyrethroid Metabolites In Human Urine. Chem Res Toxicol. 2004 Feb;17(2):218-25.
合成参考文献
摘要:Kwiecień, H. U., Science of Synthesis: Knowledge Updates, (2024) 3, 164.