- Preparation method of 4-aminophenylacetic acid medicine intermediate
-
The invention provides a preparation method of a 4-aminophenylacetic acid medicine intermediate. The preparation method comprises 1, adding concentrated sulfuric acid, concentrated nitric acid and benzyl cyanide into a reactor, carrying out a reaction process, and carrying out crystallization, filtration, water washing and re-crystallization to obtain 4-nitrophenylacetonitrile, 2, adding a sulfuric acid solution and glacial acetic acid into the 4-nitrophenylacetonitrile, carrying out heating backflow, after the reaction, pouring the reaction mixture into a reactor with ice water so that the product is crystallized and precipitated in the ice water, carrying out suction filtration to obtain white solids, carrying out re-crystallization through distilled water and glacial acetic acid, and drying the crystals to obtain 4-nitrophenylacetic acid, 3, adding 4-nitrophenylacetic acid, ethanol and skeletal nickel into a pressure reactor according to a certain ratio, carrying out a reaction process for some time, carrying out standing cooling to the room temperature, distilling to remove solvent ethanol, cooling the solution for crystallization, filtering the crystals and drying the crystals to obtain crude products, and 4, carrying out re-crystallization on the crude products through ethanol, and carrying out decoloring through active carbon to obtain light white crystals of 4-aminophenylacetic acid. The preparation method has a low cost and less side reactions and is suitable for industrial application.
- -
-
-
- A method for preparing the amino acetic acid (by machine translation)
-
The invention discloses a method for preparing the amino acetic acid, comprises the following steps: the water, ferric chloride, acetic acid mix to the nitrobenzene, in under the nitrogen atmosphere up to 60 - 90 °C, water drop [...] aqueous solution, thermal insulation 1 - 2h, the temperature crystallization, filter and filter cake, washing, drying to obtain the amino acetic acid. This invention does not produce difficult to dispose of solid waste, is free of organic solvent, the protection of the environment, mild reaction conditions, the operation is simple, and is suitable for industrial production, high yield, preparation to get amino acetic acid purity is good, for the normal and stable production of the acher he benefits help. (by machine translation)
- -
-
Paragraph 0017; 0023; 0024
(2017/01/19)
-
- Design, synthesis and biological evaluation of novel sesquiterpene mustards as potential anticancer agents
-
Several novel series of sesquiterpene mustards (SMs) bearing nitrogen mustard and glutathione (GSH)-reactive α-methylene-γ-butyrolactone groups were successfully prepared for the first time and showed excellent antiproliferative activities in vitro. Among them, compounds 2e and 2g displayed the highest antiproliferative properties with IC50 values ranging from 2.5 to 8.7 μM. The selectivity of these two compounds was evaluated by SRB method against human cancer and normal hepatic cells (HepG2 and L02). The induction of apoptosis and effects on the cell cycle distribution with compounds 2e and 2g were investigated by Hoechst 33,258 staining and flow cytometry, which exhibited that they could induce selective cell apoptosis and cell cycle arrest in HepG2 and L02 cells. In addition, further investigation showed that compounds 2e and 2g could obviously inhibit the proliferation of HepG2 cells by inducing significant DNA cross-linking and depleting GSH in cell media. The good cytotoxicity and selectivity of compounds 2e and 2g pointed them as promising leads for anticancer drug design.
- Xu, Yuan-Zhen,Gu, Xue-Yan,Peng, Shou-Jiao,Fang, Jian-Guo,Zhang, Ying-Mei,Huang, De-Jun,Chen, Jian-Jun,Gao, Kun
-
p. 284 - 297
(2015/03/30)
-
- Immunomodulatory peptides
-
The invention relates to peptides derivatized with a hydrophilic polymer which, in some embodiments, bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used in some embodiments, for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates, in further embodiments, to methods of using and methods of making the peptides of the invention.
- -
-
-
- Mild and selective hydrogenation of nitro compounds using palladium nanoparticles supported on amino-functionalized mesocellular foam
-
We present the utilization of a heterogeneous catalyst comprised of Pd nanoparticles supported on aminopropyl-functionalized siliceous mesocellular foam (Pd0-AmP-MCF) for the selective hydrogenation of aromatic, aliphatic, and heterocyclic nitro compounds to the corresponding amines. In general, the catalytic protocol exclusively affords the desired amine products in excellent yields within short reaction times with the reactions performed at room temperature under ambient pressure of H2. Moreover, the reported Pd nanocatalyst displayed excellent structural integrity for this transformation as it could be recycled multiple times without any observable loss of activity or leaching of metal. In addition, the Pd nanocatalyst could be easily integrated into a continuous-flow device and used for the hydrogenation of 4-nitroanisole on a 2.5 g scale, where the product p-anisidine was obtained in 95% yield within 2 h with a Pd content of less than 1 ppm.
- Verho, Oscar,Gustafson, Karl P. J.,Nagendiran, Anuja,Tai, Cheuk-Wai,B?ckvall, Jan-E.
-
p. 3153 - 3159
(2015/02/03)
-
- A novel method for the synthesis of actarit
-
The specific synthetic route to synthesize the actarit (4-acetyl-amino phenylacetic acid) by acylation was designed in which p-amino benzaldehyde (a) and nitromethane (b) was used as the raw materials, through Knoevenagel reaction. The selective reduction of potassium borohydride and p-amino phenylacetic acid to be oxidated under the acidic conditions. After optimization of the synthetic conditions, the yield of each step was more than 85 %. The synthesized compound was confirmed by the elemental analysis and nuclear magnetic resonance. Because of the readily available raw materials, simple operations, high yield and avoiding highly toxic reagents in the synthesis of actarit (4-acetyl-amino phenylacetic acid), the synthetic route is suitable for the industrial production.
- Zhou, Li-Yi,Yang, Jun,Yan, Xi-Qing,Pan, Yan-Juan,Wu, Feng,Zhang, Jing,Yan, Fu-Lin,Lu, Guang-Zhou
-
experimental part
p. 1538 - 1540
(2012/10/07)
-
- Synthesis and hydrolytic evaluation of acid-labile imine-linked cytotoxic isatin model systems
-
In this study a series of isatin-based, pH-sensitive aryl imine derivatives with differing aromatic substituents and substitution patterns were synthesised and their acid-catalysed hydrolysis evaluated. These derivatives were functionalised at the C3 carbonyl group of a potent N-substituted isatin cytotoxin and were stable at physiological pH but readily cleaved at pH 4.5. Observed rates of hydrolysis for the embedded imine-acid moiety were in the order para-phenylpropionic acid > phenylacetic acid (para > meta) > benzoic acid (meta > para). The ability to fine-tune hydrolysis rates in this way has potential implications for optimising imine linked, tumour targeting cytotoxin-protein conjugates.
- Matesic, Lidia,Locke, Julie M.,Vine, Kara L.,Ranson, Marie,Bremner, John B.,Skropeta, Danielle
-
experimental part
p. 1771 - 1778
(2011/04/17)
-
- PROCESS FOR THE PREPARATION OF TRANS 4-AMINO-CYCLOHEXYL ACETIC ACID ETHYL ESTER HCL
-
The invention relates to a process for the preparation of trans 4-amino-cyclohexil ethyl acetate HCl wherein d) hydrogenating 4-nitrophenyl acetic acid in a protic solvent at a temperature between 40-50° C. in the presence of Pd/C under 0.1-0.6 bar overpressure, and e) further hydrogenating the 4-aminophenyl acetic acid obtained in situ in step a) at a temperature between 50-60° C. under 1-4 bar overpressures, then f) heating to reflux the 4-aminocyclohexil acetic acid obtained in step b) for 1-3 hours in hydrochloric ethanol, and if desired after removing the solvent acetonitrile was added to the residue obtained and distilled off.
- -
-
Page/Page column 2
(2011/12/12)
-
- NOVEL MULTIMERIC MOLECULES, A PROCESS FOR PREPARING THE SAME AND THE USE THEREOF FOR MANUFACTURING MEDICINAL DRUGS
-
The invention relates to a compound of the formula (I): in which k and j are independently 0 or 1, Y is a macrocycle in which the cycle includes 9 to 36 carbon atoms and is functionalised by three amino functions and by a chain for attaching the spacer arm Z via an X bond, Rc is a binding pattern with a receptor of the TNF superfamily, X is a chemical function for binding the Y group to the space arm, and Z is a bi-, tri- or tetra-functional spacer arm.
- -
-
-
- NOVEL MULTIMERIC CD40 LIGANDS, METHOD FOR PREPARING SAME AND USE THEREOF FOR PREPARING DRUGS
-
The invention concerns a compound of formula (I), wherein Y represents a macrocycle whereof the cycle comprises 9 to 36 atoms, and is functionalized by three amine or COOH functions; Rc represents a group of formula H—Xa—Xb—Xc—Xd—Xe—(Xf)i—, wherein i represents 0 or 1, Xn is in particular selected among lysine, arginine, ornithine residues, Xb is in particular selected among glycine, asparagine, L-proline or D-proline residues, Xc et Xd are in particular selected among tyrosine, phenylalanine or 3-nitrotyrosine residues, Xe et Xf are in particular selected among the following amino acid residues: NH2—(CH2)n—COOH, n ranging from 1 to 10 or NH2—(CH2—CH2—O)m—CH2CH2COOH, m ranging from 3 to 6, provided that one at least of the amino acid residues Xa, Xb, Xc and Xd is different from the corresponding amino acid in the sequence of the natural CD40 143Lys-Gly-Tyr-Tyr146 fragment
- -
-
-
- One step hair coloring compositions using salts
-
A hair coloring composition comprising the following two compositions which are mixed just prior to application to the hair: (a) a composition comprising a water-soluble peroxygen oxidizing agent; and (b) a composition comprising one or more oxidative hair coloring agents selected from the group consisting of an aromatic diamine, an amino phenol, a naphthol, a polyhydric phenol, a catechol and mixtures thereof; wherein the composition comprising one or more oxidative hair coloring agents further comprises al least one water soluble carbonate releasing salts; and optionally a water soluble ammonium salt, is described.
- -
-
-
- Transition metal complexes as dye forming catalysts in hair coloring compositions
-
A hair coloring composition comprising a first composition which comprises: (a) a dye forming transition metal salt or complex; which is first applied to the hair; and a second composition which comprises the following two compositions which are mixed just prior to application to the hair: (a) a composition comprising a water-soluble peroxygen oxidizing agent; and (b) a composition comprising one or more oxidative hair coloring agents selected from the group consisting of an aromatic diamine, an aminophenol, a polyhydric phenol a catechol and mixtures thereof.
- -
-
-
- Hair colouring and conditioning compositions
-
A hair colouring and conditioning composition comprising: (a) a hair colouring agent; and (b) a hair conditioning agent; wherein the composition provides an Average Combing Index Value of greater than 1.2 as measured by the Combing Technical Test Method. The products can provide excellent hair colouring together with excellent conditioning, reduced hair damage, brittleness and dryness, and is convenient and easy to use.
- -
-
-
- Hair conditioning compositions and their use in hair colouring compositions
-
The present invention relates to a hair care composition comprising a aminofunctional polysiloxane having a specified average effective particle size which provides improved durable conditioning particularly when utilised in conjunction with a hair colouring composition.
- -
-
-
- HAIR COLORING COMPOSITIONS
-
A hair coloring composition comprising: (a) from about 0.0003 moles (per 100 g of composition) to less than about 0.09 moles (per 100 g of composition) of an inorganic peroxygen oxidizing agent; and (b) an oxidative hair coloring agent; wherein the pH of each of (a) and (b) is in the range of from about 1 to about 6 and wherein the combined mixture of (a) and (b) has a pH in the range of from about 1 to about 6. The products can provide excellent hair coloring and in-use efficacy benefits including excellent initial color and good wash fastness in combination with reduced hair damage at low pH.
- -
-
-
- HAIR COLORING COMPOSITIONS
-
A hair coloring composition comprising: (a) a preformed organic peroxyacid oxidising agent; and (b) an oxidative hair coloring agent; wherein the pH of each of components (a) and (b) is in the range of from about pH 1 to less than about pH 7 and wherein the pH of the composition is in the range of from about pH 1 to less than about pH 7. The products can provide excellent hair coloring and in-use efficacy benefits including excellent initial color and good wash fastness in combination with reduced hair damage at low pH.
- -
-
-
- Adhesion receptor antagonists III
-
Novel oxazolidinone derivatives of the formula I STR1 in which R1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H2 N--CH2 --, A2 N--CH2 --, H2 N--C(=NH)--, H2 N--C(=NH)--NH--, H2 N--C(=NH)--NH--CH2 --, HO--NH--C(=NH)-- or HO--NH--C(=NH)--NH--, X is O, S, SO, SO2, --NH-- or --NA--, B is STR2 or STR3 A is alkyl having from 1 to 6 C atoms, R2 is H, A, Li, Na, K, NH4 or benzyl, R3 is H or (CH2)n --COOR2, E is, in each case independently of each other, CH or N, Q is O, S or NH, m is 1, 2 or 3, and n is 0, 1, 2 or 3, and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.
- -
-
-
- Electronic Substituent Effects in the Nitrilase-Catalyzed Hydrolysis of Para-Substituted Benzyl Cyanides
-
The initial rates of the nitrilase (Novo)-catalyzed hydrolysis of a series of para-substituted benzyl cyanides (R = NO2, Cl, OCH3, OH, NH2) were found to be susceptible to the nature of the para-substituent of the substrate and a Hammett-type linear free energy correlation was observed with ρ = 0.96.In a separate study, effective solubilization of substituted benzyl cyanide substrates having electron-donating groups (OH, NH2, OCH3) was achieved upon mixing with β-cyclodextrin to form 1:1 mol ratio inclusion complexes, but para-substituted benzyl cyanides with electron-withdrawing groups (Cl, NO2) were not fully solubilized under the same conditions.In addition, it was shown that the presence of β-cyclodextrin not only had no inhibitory effect on the enzyme activity, but it actually increased the initial rate of hydrolysis of the unsubstituted benzyl cyanide:β-cyclodextrin inclusion complex.However, the initial rates of hydrolysis were observed to be smaller when β-cyclodextrin was added to the para-substituted benzyl cyanides.
- Geresh, Shimona,Giron, Yakir,Gilboa, Ygal,Glaser, Robert
-
p. 10099 - 10102
(2007/10/02)
-
- Catalytic Transfer Hydrogenation of Aromatic Nitro Compounds Employing Formic Acid in Presence of Palladium Black
-
Aromatic nitro compounds like nitrophenols and nitroamines can be conveniently reduced by catalytic transfer hydrogenation employing formic acid in the presence of palladium black.The reaction rate is greatly enhanced by the addition of a small quantity of sodium formate.
- Sivanandaiah, K. M.,Gurusiddappa, S.,Gowda, D. Channe
-
-
- Protection of Primary Amines as N-Substituted 2,5-Dimethylpyrroles
-
Protection of primary amine group is achieved by incorporating it into an N-substituted 2,5-dimethylpyrrole system.The method affords protection against strong bases and nucleophiles, heating with concentrated alkali, standard mineral acid work-up conditions, and various other reagents.Phenyl-, pyridil-, thiazolyl-, and alkyl-amines have been studied.All give trisubstituted pyrroles in high yield (>80percent) by reaction with hexane-2,5-dione.The pyrroles from the first three types are stable to storage; even the N-alkyl compounds can be used without difficulty.Regeneration of the amine group, by treatment with hydrxylamine hydrochloride, is efficient (80percent yield) with the phenyl, pyridyl, and alkyl compounds but less satisfactory (60 - 65percent generally but down to 25percent in two cases) with the thiazolyl derivatives.
- Bruekelman, Stephen P.,Leach, (Miss) Susan E.,Meakins, G. Denis,Tirel, Malcolm D.
-
p. 2801 - 2807
(2007/10/02)
-
- A GENERAL PROCEDURE FOR MILD AND RAPID REDUCTION OF ALIPHATIC AND AROMATIC NITRO COMPOUNDS USING AMMONIUM FORMATE AS A CATALYTIC HYDROGEN TRANSFER AGENT
-
Various aliphatic and aromatic nitro compounds were selectively and rapidly reduced to their corresponding amino derivatives in very good yield using anhydrous ammonium formate as a catalytic hydrogen transfer agent.
- Ram, Siya,Ehrenkaufer, Richard E.
-
p. 3415 - 3418
(2007/10/02)
-
- Protection of Primary Amines as N-Substituted 2,5-Dimethylpyrroles
-
Protection of a primary amine group against attack by organic or aqueous solutions of strong bases or nucleophiles is achieved by incorporation into an N-substituted 2,5-dimethylpyrrole system from which the amine group is regenerated by treatment with hydroxylamine hydrochloride.
- Breukelman, Stephen P.,Meakins, G. Denis,Tirel, Malcolm D.
-
p. 800 - 801
(2007/10/02)
-
- Pyrazol-1-ylphenylacetic acids
-
Pyrazol-1-ylphenylacetic acids of the formula STR1 wherein R1, R2 and R3 are the same or different and denote a hydrogen atom or a halogen atom, R4 denotes a hydrogen atom or an alkyl group, A B denotes a carbon-carbon single or double bond, and their salts are pharmacologically active and are useful as medicaments. Medicament compositions are produced therefrom. Their functional carboxylic acid derivatives and other new intermediates are used in their preparation.
- -
-
-
- Enzyme-activated oxidative process for coloring hair
-
An enzyme-based oxidative process for coloring hair wherein the hair is exposed to a solution having a pH of about 4 to about 10 and containing hydrogen peroxide, soybean peroxidase enzyme and one or more oxidation dye precursors.
- -
-
-
