- Cefprozil refining method
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The invention discloses a cefprozil refining method. The method includes: (1) dissolving a crude cefprozil product in a mixed solvent of deionized water, ethanol and dichloromethane, conducting heating reflux dissolution to prepare a saturated or supersaturated solution; (2) performing cooling to 20-30DEG C, adding activated carbon for decolorization, conducting filtration, cooling the filtrate to5DEG C-10DEG C, performing crystallization for 1h, conducting cooling to 0DEG C-5DEG C, and performing crystal growing; (3) conducting filtering, and performing leaching with ethanol to obtain a white solid; and (4) placing the white solid obtained by step (3) in a vacuum drying box, conducting vacuum pumping, and performing drying for 3h or more, thus obtaining cefprozil crystals. The refining method provided by the invention remarkably improves the product quality, and is simple in operation, thus being suitable for industrial production.
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Paragraph 0027-0029; 0034-0036; 0041-0043
(2019/12/02)
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- AGONISTS THAT ENHANCE BINDING OF INTEGRIN-EXPRESSING CELLS TO INTEGRIN RECEPTORS
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A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of α4β1, α5β1, α4β7, αvβ3 and αLβ2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
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Page/Page column 70
(2012/06/01)
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- Method of preparing cephalosporins using 4-hydroxyphenylglycine derivatives
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High purity cephalosporin compound can be easily prepared in a high yield by a process comprising the steps of: reacting a cephem compound with a 4-hydroxyphenylglycine derivative.
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- Anti-cancer compounds
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Cyclopentaquinazoline of the formula (I): STR1 wherein R1 is hydrogen, amino, C1-4 alkyl, C1-4 alkoxy, C1-4 hydroxyalkyl or C1-4 fluoroalkyl; wherein R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and wherein R3 is a group of the formula: in which A1, A2, Y1 and Ar2 are defined in claim 1; or a pharmaceutically acceptable salt or ester there of are of therapeutic value particularly in the treatment of cancer.
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- A NOVEL SYNTHESIS OF (+/-)-3-AMINONOCARDICINIC ACID
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(+/-)-3-Aminonocardicinic acid (3-ANA, 2), which is an important material for the synthesis of nocardicin A (1) and other biologically active analogues, has been synthesized by the application of a new method for the synthesis of α-methylene-β-lactams.
- Chiba, K.,Mori, M.,Ban, Y.
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p. 387 - 392
(2007/10/02)
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- Derivatives of L- and DL-4-hydroxyphenylglycine
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L- and DL-isomers of compounds of the formula STR1 and the pharmaceutically acceptable salts thereof, wherein R is hydrogen or methyl; R1 is alkynyl, alkenyl or cycloalkyl, each having from three to seven carbon atoms or alkyl having from one to six carbon atoms which may optionally be substituted by one or more groups selected from hydroxy, alkoxy, carboxy, amino, monoalkylamino, dialkylamino, phenyl and phenoxy, any such phenyl or phenoxy being optionally substituted with one or more hydroxy, alkyl or alkoxy groups, said alkyl and alkoxy optional substituents having from one to six carbon atoms; provided that R1 is other than 4-hydroxy-α-carboxybenzyl or 4-methoxy-α-carboxybenzyl. Said compounds are useful in treating diseases and conditions characterized by reduced blood flow, oxygen availability or carbohydrate metabolism in the cardiovascular system. The D-isomers of the compounds of formula (II) are substantially inactive in treating such diseases and conditions.
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- 7[2(2,3 Dioxopiperazin-1-yl-carbonylamino)substituted 2 phenylacetamido]-3-2'-thiadiazolyl cephalosporanic acid derivatives
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Disclosed are broad spectrum antibiotics derived from 7-[D(-)-α-(4-alkyl-2,3-dioxopiperazin-1-yl-carbonylamino)-substitutedphenylacetamido]-3-(5-substituted or unsubstituted-1,3,4-thiadiazol-2-yl-thiomethyl)-3-cephem-4-carboxylic acids and salts thereof.
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- Derivatives of 7-(cyclized)phenylglycyl-3-triazolo-thio methyl cephalosporin
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Compounds of the formula STR1 wherein A is hydrogen, hydroxy, methyl or methoxy, R1 is hydrogen, sodium or potassium, and R2 is 1,2,3-triazol-5-yl, such group being unsubstituted or substituted with one or two lower alkyl groups of o
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- Process for preparing substituted glycines
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A new process is disclosed for the preparation of N-acyl-α-aromatic and N-acyl-α-heteroaromatic glycines by reaction of an α-ester or ether of an N-acylglycine ester or acid with an aromatic or heteroaromatic compound. Also disclosed are new intermediates for preparing N-acyl-α-aromatic and N-acyl-α-heteroaromatic glycines.
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- Crystalline sesquihydrate of 7-[D-α-amino-α-(p-hydroxyphenyl)acetamido]-3-(1,2,3-triazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid
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The crystalline sesquihydrate of 7-[D-α-amino-α-(p-hydroxyphenyl)acetamido]-3-(1,2,3-triazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid is prepared and found to be a stable useful form of the cephalosporin antibiotic particularly advantageous for pharmaceutical formulations.
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