专利号:US-11274081-B2 优先权日:2016-05-30 标 题:Process for the synthesis of ivacaftor 发明人:REDDY DUMBALA SRINIVASA; KULKARNI AMOL ARVIND; NATARAJAN VASUDEVAN; SHARMA MRITYUNJAY KESHAVPRASAD 权利人:COUNCIL SCIENT IND RES 摘要:The present disclosed an improved process for the synthesis of ivacaftor starting from indole acetic acid ester which can be performed in batch as well as continuous flow synthesis. The present invention further disclosed to a continuous process for the synthesis of compound of formula (II) or formula (III) from compound of formula (I) in continuous flow reactor.
专利号:US-2024384319-A1 优先权日:2021-09-17 标题 :Synthesis of Oligonucleotides 发明人:LOVELOCK SARAH 权利人:UNIV MANCHESTER 摘要:The present invention relates to a novel method for oligonucleotide synthesis, using a catalytic primer-template, e.g. a hairpin primer, to achieve multiple rounds of oligonucleotide synthesis and dissociation from the template in the same reaction, such that at the end of the reaction the amount of oligonucleotide generated is greater than the amount of template provided in the reaction. The primer contains a cleavable site and the reaction is carried out in a single mixture with a cleavage agent. The cleavable site may be an inosine and the agent an endonuclease V.
专利号:US-11332444-B2 优先权日:2018-04-25 标题:Method for the hydrolysis of quinolonecarboxylic esters 发明人:FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE 权利人:BAYER ANIMAL HEALTH GMBH 摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.
专利号:US-12252473-B2 优先权日:2022-04-18 标 题:Preparation methods of quinolone compounds and intermediates thereof 发明人:LEI JIE; CHEN ZHONGZHU; XU ZHIGANG; TANG DIANYONG; XU JIAYU; ZHOU HAOYI; XIA DANDAN; LIU YAO; CAO YIHUA; LUO JIE 权利人:UNIV CHONGQING ARTS & SCIENCES 摘要:The present application relates to processes for the preparation of quinolone compounds and intermediates thereof, particularly to processes for the preparation of quinolones and pharmaceutical intermediates of the quinolones. In particular, the present application provides a process for the preparation of a compound of Formula I, and a process for the synthesis of quinolone compounds using the compound of Formula I as an intermediate. The process for the preparation of the compound of Formula I comprises the steps of:reacting a compound of Formula A with R5NH2 and R6Cl in the presence of a base to form the compound of Formula I,
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-8093381-B2 优先权日:2007-05-24 标题:Method of synthesis of fluoroquinolones 发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS 权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX 摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.
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