4,5-二氨基-6-氯嘧啶置于palladium On Activated Charcoal,水体系中,化学反应生成4,5-二氨基嘧啶 参考文献:The Synthesis And Properties Of 6-Chloropurine And Purine1 标题:The Synthesis And Properties Of 6-Chloropurine And Purine1 摘要: Doi:10.1021/ja01652A062
专利信息
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:US-8551237-B2 优先权日:2007-12-10 标 题 :Synthesis of colorants in mixing apparatus 发明人:LOEBEL JOHANNES 权利人:LOEBEL JOHANNES; BASF SE 摘要:A process for preparing colorants of the general formula (Ia), (Ib) or (Ic) n nor mixtures thereof, comprises reactingn (a) tetracarboxylic acids or their functional derivatives with (b) at least one compound selected fromn i. aliphatic amines, ii. aromatic amines, iii. aliphatic diamines, iv. aromatic diamines, n (c) optionally in the presence of further additives, (d) optionally in the presence of wetting agentsn nin a mixing apparatus. These colorants are useful for coloration of macromolecular organic and inorganic materials of natural and synthetic origin.
专利号:US-4080325-A 优先权日:1976-11-17 标 题 :Synthesis of methotrexate 发明人:ELLARD JAMES A 权利人:US HEALTH EDUCATION & WELFARE 摘要:The present invention consists of three process improvements in the so-called multi-step Piper-Montgomery process designed especially to produce the antifolate methotrexate which is closely related to both aminopterin and folic acid. 2,4,5,6-tetraaminopyrimidine sulfite is one starting material and is usually produced in the form of the bisulfite in an acetate buffer. The present modification positively produces the hydrochloride from the bisulfite and eliminates the acetate buffer utilized in prior art processes. Subsequently, a pteridine ring is formed from the pyrimidine hydrochloride using dihydroxyacetone at pH 5.5±0.2 to form the second ring. This strict pH control together with the use of hydrochloride salt minus the acetate buffer assists in preferentially favoring the formation of 2,4-diamino-6-hydroxymethylpteridine. Subsequently the 6-hydroxy-methyl compound is converted to the hydrobromide acid salt and reacted with three moles of a triphenyl dibromophosphorane and phosphazine protecting groups are formed on the amine groups of the pteridine ring as the 6-hydroxymethyl group is transformed to 6-bromomethyl, a key intermediate. The present process leaves the protecting phosphazine groups on the primary amino groups to discourage side reactions during subsequent alkylation of the other major reactant, ethyl N-(p-methylaminobenzoyl)-L-glutamate. Furthermore, ethyl N-(p-methylaminobenzoyl)-L-glutamate, the other reactant, is uniquely produced for the present multi-step reaction by a process proceeding from ethyl N-(p-trifluoromethylaminobenzoyl)-L-glutamate by utilizing an alkali metal hydroxide in a lower (C 1 -C 6 ) alkanol wherein the protective trifluoroacetyl groups are removed. This step uses a special mixture preferably of an alkali metal hydroxide in ethanol and optimally 1 equivalent of KOH in 20% ethanol at or below ambient temperature where the mixture is added slowly to keep the reaction pH below 9. The combination of these improvements results in the increase of an overall yield of methotrexate from the named starting reactants from about 25% to approximately 40-50%.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:US-11845891-B2 优先权日:2014-07-02 标 题 :Chemical synthesis of hybrid inorganic-organic nanostructured corrosion inhibitive pigments and methods 发明人:ZHANG WEILONG 权利人:UNITED TECHNOLOGIES CORP; RTX CORP 摘要:A method for preparing a hybrid inorganic-organic nanostructured inhibitive pigment, includes premixing a first stock solution containing one or more cations and a second stock solution containing one or more oxoanions to form a premixture under pH control in the presence of polymers as surface modifiers. The premixture is then reacted to form a slurry. The slurry is then quenched to separate nanoparticles from the slurry, followed by surface functionalization in organic inhibitors.
专利号:US-8334386-B2 优先权日:2007-07-03 标题:Aqueous synthesis of perylene pigments 发明人:LOEBEL JOHANNES; STOHR ANDREAS 权利人:LOEBEL JOHANNES; STOHR ANDREAS; BASF SE 摘要:A process for preparing perylene pigments of the general formula (Ia) or (Ib) n nor mixtures thereof, by reacting perylenetetracarboxylic acids or functional derivatives thereof with aromatic diamines, where R 1 , R 2 may be the same or different and may each independently be phenylene, naphthylene or pyridylene, where R 1 , R 2 may each be mono- or polysubstituted by C 1 -C 22 -alkyl, C 3 -C 22 -alkenyl, C 1 -C 22 -alkoxy, hydroxyl and/or halogen, X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 may be the same or different and may each independently be hydrogen or halogen, wherein the reaction is performed in the presence of a secondary or tertiary amine in an aqueous reaction medium.
参考标题:Water-Based Conditions For The Microscale Parallel Synthesis Of Bicyclic Lactams 作者:Sandra Malaquin,Mouhamad Jida,Justin Courtin,Guillaume Laconde,Nicolas Willand,Benoit Deprez,Rebecca Deprez-Poulain |发布日期:2013.2 摘要:A Mixture Of Ethanol And Water Yields The Expected Lactams, We Exemplified The Reaction And Procedure With The Preparation Of A Library Of 80 Members. Our Synthesis Scheme Is Validated For Synthesis Scales From 1 To 100 Mg. Therefore, It Can Be Used Both To Produce Rapidly Test Samples For Hts As Well As To Prepare Intermediates For The Synthesis Of More Elaborated Nature-Inspired Compounds.
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 430. 摘要:A. Albert. J. Chem. Soc. 1955, 2690. 摘要:G.B. Barlin and W. Pfleiderer. J. Chem. Soc., B 1971.