专利号:US-2006111369-A1 优先权日:2004-11-10 标 题:Synthesis, characterization and biological action of optically active isomers of floxacins 发明人:SOMBERG JOHN C; RANADE VASANT V 权利人:SOMBERG JOHN C; RANADE VASANT V 摘要:Disclosed herein is the method for synthesis and separation of enantiospecific isomers of floxacins. These isomers can be used to study the antibacterial action, as well as cardiac effects, such as arrhythmogenic activity, QT internal prolongation and dispersion, and Ikr inhibition in humans. A method for the identification of chiral isolates of the floxacins that are devoid or possess less QT prolonging action and thus cause less arthropathy especially of the Torsades de pointes variety. Also disclosed are methods for assaying these isomeric compounds present in the biological fluids.
专利号:US-9006231-B2 优先权日:2008-03-03 标 题:Cephalotaxus esters, methods of synthesis, and uses thereof 发明人:GIN DAVID Y; WILMOT JEREMY; DJABALLAH HAKIM 权利人:SLOAN KETTERING INST CANCER 摘要:The present invention provides novel cephalotaxus esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer.
专利号:US-3772363-A 优先权日:1961-08-18 标题:3,4,10-trioxo octahydroanthracene-2-aminoacetic acids and derivatives thereof 发明人:CONOVER L; WOODWARD R 权利人:PFIZER 摘要:THE TOTAL SYNTHESIS OF TETRACYCLINE-TYPE ANTIBIOTICS BY A MULTISTEP PROCESS BEGINNING WITH 3,4,10-TRIOXO-1,2,3,4,4A, 9,9A,10-OCTAHYDROANTHRACENES COMPRISING: (1) AN ALDOL CONDENSATION WITH A GLYOXALIC ACID ESTER TO GIVE A 2-CARBOXYMETHYLIDENE - 3,4,10 - TRIOXO - 1,2,3,4,4A,9,9A,10OCTAHYDROANTHRACENE ESTER; (2) MICHAEL REACTION OF SAID ESTER WITH AN AMINE TO PRODUCE A 3,410-TRIOXI-1,2,3,4,4A, 9,9A,10-OCTAHYDROANTHRACENE-2-(AMINO) ACETIC ACID ESTER; (3) CONVERSION OF THE TRIKETONE TO THE CORRESPONDING 4,10DIKETONE BY (A) SELECTIVE REDUCTION OF THE MICHAEL REACTION PRODUCT TO THE CORRESPONDING 3-HYDROXY COMPOUND, FOLLOWED BY CONVERSION OF THE 3-HYDROXY COMPOUND TO THE CORRESPONDING 3-FORMYLOXY COMPOUND AND REMOVAL OF THE 3-FORMYLOXY GROUP BY TREATMENT WITH ZINC DUST TO GIVE A 4,10-DIOXO-1,2,3,4,4A,9,9A810-OCTAHYDROANTHRACENE-2-(AAMINO) ACETIC ACID ESTER; OR (B) CONVERSION OF THE HYDROCHLORIDE SALT OF THE MICHAEL REACTION PRODUCT TO A LACTONE BY REACTION WITH P-TOLUENE-SULFONIC ACID AND TREATMENT OF THE LACTONE WITH ZINC DUST FORMIC ACID; (4) CONVERSION OF THE 4,10-DIKEOT-1,2,3,4,4A,9,9A,10-OCTAHYDROANTHRACENE2-(A-AMINO) ACETIC ACID TO MIXED ANHYDRIDE; (5) FOLLOWED BY ACYLATION OF A MALONIC ACID ESTER WITH THE MIXED ANHYDRIDE; (6) CYCLIZATION OF THE ACYL MALONATE DERIVATIVE TO A 12A-DEOXYTETRACYCLINE WHICH IS THEN HYDROXYLATED TO A TETRACYCLINE. THE PREPARATION OF THE 3,4,10-TRIOXO-1,2,3, 4,4A,9,9A,10-OCTAHYDROANTHRACENES FROM BENZOYL HALIDES BY (A) FRIEDEL-CRAFTS REACTION OF A BENZOYL HALID WITH A PYROCATECHOL ETHER, E.G., A DI-(LOWER) ALKYL ETHER, TO PRODUCE A 3,4-DI-(LOWER) ALKOXYBENZOPHENONE; (B) CONVERSION OF THE BENZOPHENONE BY PARTIAL OR COMPLETE REDUCTION OF THE CARBONYL GROUP BY CHEMICAL OR CATALYTIC METHODS TO A 3,4-DI-(LOWER) ALKOXY DIPHENYL METHANOL OR 3,4-DI(LOWER) ALYKOXY DIPHENYL METHANE; OR TO A 3,4-DI-(LOWER) ALKOXY DIPHENYL ALKANE VIA A GRIGNARD REACTION AND REDUCTION OF THE THUS-PRODUCED ALKANOL; (C) OXIDATION OF THE 3,4-DI (LOWER) ALKOXY DIPHENYL ALKANE, OR THE CORRESPONDING DIHYDROXY COMPOUND, TO A DIENEDIOIC ACID ESTER OR DIENEDIOIC ACID; (D) HYDROGENATION OF THE DIENEDIOIC ACID COMPOUND TO A BENZYL ALIPIC ACID DERIVATIVE; (E) CYCLIZATION OF SAID COMPOUND TO A 2-(2-CARBALKOXYETHYL)-4-TETRALONE BY MEANS OF DEHYDRATING OR DEHYDROHALOGENATING AGENTS; (F) CYCLIZATION OF THE 4-TETRALONE DERIVATIVES BY CONDENSATION WITH A DIALKYLOXALATE TO GIVE A 2-CARBALKOXY 3,4,10-TRIOXOOCTAHYDROANTHRACENE; AND (G) REMOVAL OF THE 2-SUBSTITUENT BY DECARBOXYLATION. THE INTERMEDIATES AND FINAL PRODUCTS ARE USEFUL AS BACTERICIDES AND/OR CHELATING AGENTS.
专利号:CN-102977089-A 优先权日:2012-12-06 标 题:A preparation method of key raw material for synthesis of high-purity cefdinir antibiotic 7-position side chain
专利号:CN-101321741-A 优先权日:2005-12-05 标题 :Process for the selective synthesis of enantiomers of substituted 1-(2-amino-1-phenyl-ethyl)-cyclohexanols