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3-nitrophthalic acid anhydride 3-nitrophthalic acid 2-amino-6-methylbenzoic acid hydrogenchloride 3-Methoxybenzoic acid 3-hydroxyphthalic acid 3-iodophthalic acid 3-benzoylamino-phthalic acid 邻苯二甲酸置于barium Dihydroxide,硫酸,氨,硝酸,Iron(II) Sulfate体系中,化学反应生成 3-氨基苯二甲酸
参考文献:Onnertz,Chemische Berichte,1901,Vol. 34,P. 3744
标题:Onnertz,Chemische Berichte,1901,Vol. 34,P. 3744
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专利信息
专利号:US-6051704-A
优先权日:1996-07-22
标题:Synthesis of macrocyclic tetraamido-N ligands
发明人:GORDON-WYLIE SCOTT W; COLLINS TERRENCE J
权利人:UNIV CARNEGIE MELLON
摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.
专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人:MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
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-5866335-A
优先权日:1994-06-24
标题:Preparation of derivatized 10,10'-substituted-9,9'-biacridine luminescent molecules and signal solutions
发明人:KATSILOMETES GEORGE W; HO PAK T
权利人:KATSILOMETES GEORGE W
摘要:The synthesis of 10,10'-substituted-9,9'-biacridine molecules and their derivatives is disclosed. These molecules are shown to catalyze the production of light by chemiluminescence in the presence of a signal solution having at a pH from about 10.0 to about 14.0, at a concentration effective for producing a chemiluminescent signal, a chelating agent, a sulfoxide, a reducing sugar, an oxidant or combination of oxidants, an alcohol and aqueous sodium tetraborate. These 10,10'-substituted-9,9'-biacridines are used alone or attached to haptens or macromolecules and are utilized as labels in the preparation of chemiluminescent, homogeneous or heterogeneous assays. They are also used in conjunction with other chemiluminescent label molecules to produce multiple analyte chemiluminescent assays.
专利号:US-2007031854-A1
优先权日:1999-02-01
标题:Novel 10,10'-substituted-9,9'-biacridilidine luminescent molecules their preparation and uses
发明人:KATSILOMETES GEORGE W
权利人:KATSILOMETES GEORGE W
摘要:Novel symmetric, uniformly symmetric and asymmetric 10,10′-substituted-9,9′-biacridines and the synthesis of such symmetric, uniformly symmetric and asymmetric 10,10′-substituted-9,9′-biacridine molecules and their derivatives is disclosed. These molecules are shown to produce light by luminescence in the presence of signals. These symmetric, uniformly symmetric or asymmetric 10,10′-substituted-9,9′-biacridines are used alone or attached to haptens or macromolecules and are utilized as labels in the preparation of iluminescent homogeneous and heterogeneous assays. They are also used in conjunction with other label molecules to produce multiple analyte assays.
专利号:US-6011152-A
优先权日:1996-07-22
标 题 :Synthesis of macrocyclic tetraamido-N ligands