专利号:US-9556140-B2 优先权日:2013-01-26 标 题 :Approach for synthesis of catechins 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; RAI KUMAR SANTOSH; TRIPATHI VINAYAK; PATIL ISHWAR RAKESH 权利人:SPHAERA PHARMA PRIVATE LTD 摘要:A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.
专利号:US-6455680-B1 优先权日:2000-12-21 标 题 :Methods utilizing aryl thioimines in synthesis of erythromycin derivatives 发明人:LUKIN KIRILL A 权利人:ABBOTT LAB 摘要:An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
专利号:US-9428482-B2 优先权日:2011-01-27 标 题 :Process for synthesis of polyphenols 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE; SPHAERA PHARMA PTE LTD 摘要:The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
专利号:US-6198000-B1 优先权日:1997-07-07 标 题:Intermediates useful in the synthesis of quinoline antibiotics 发明人:HAWKINS JOEL M 权利人:PFIZER 摘要:A process for preparing a compound of the formula n wherein R 1 , m, o and p are described below, which comprises adding a base of the formula n wherein R 2 , R 3 and R 4 are as described below, to a solution comprising a compound of the formula n wherein R 1 , m, o and p are as described below, and a halonitromethane of the formula O 2 NCH 2 X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R 2 is butyl, R 3 is hydrogen and each R 4 is t-butyl.
专利号:US-5298629-A 优先权日:1992-03-02 标题 :Intermediates in the synthesis of quinoline antibiotics 发明人:BRAISH TAMIN F 权利人:PFIZER 摘要:This invention relates to compounds of the formulae ##STR1## wherein R and X are defined as below. These compounds are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids having antibacterial activity.
专利号:US-6057455-A 优先权日:1996-07-09 标题 :Preparation of intermediates useful in the synthesis of quinoline antibiotics 发明人:HAWKINS JOEL M 权利人:PFIZER 摘要:A process for preparing a compound of the formula ##STR1## wherein R 1 , m, o and p are described below, which comprises adding a base of the formula ##STR2## wherein R 2 , R 3 and R 4 are as described below, to a solution comprising a compound of the formula ##STR3## wherein R 1 , m, o and p are as described below, and a halonitromethane of the formula O 2 NCH 2 X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R 2 is butyl, R 3 is hydrogen and each R 4 is t-butyl.