专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-6987186-B2 优先权日:2003-01-28 标 题 :Synthesis of small particle size quinacridone of beta crystal phase 发明人:COLE DAMIEN THURBER; JEGANATHAN SURULIAPPA GOWDER; HE YINGXIA 权利人:CIBA SC HOLDING AG 摘要:The present invention relates to a process for the synthesis of beta-quinacridone by oxidation in the presence of selected additives that promote the formation of the desired crystal phase and particle size.
专利号:WO-2013144924-A1 优先权日:2012-03-29 标 题:An improved process for the synthesis of strobilurin fungicides viz trifloxystrobin and kresoxim-methyl 发明人:KAMARAJ PASUMPON; SATAM VIJAY SHRIKANT; AJJANNA MAHALINGAPPA SRIDHARA; NANDI TAPASKUMAR; BOBADE ANNA; SHINDE RAVINDRA; NAIK PARAG; MOHITE DHANAJI; KADAM SUBHASH; HINDUPUR RAMA MOHAN; PATI HARI NARAYAN; MANE AVINASH; VADIRAJ SUPHALA GOPINATH; VENKATESH PRABHU MOODBIDRI 权利人:RALLIS INDIA LTD 摘要:The present invention relates to an improved process for the synthesis of E -isomer of compound of formula (5). It further relates to the conversion of formula (5), wherein R is H, to Intermediate (I) and subsequently to substantially pure Trifloxystrobin, compound of formula (I) in good yield.
专利号:US-6342582-B1 优先权日:1989-12-04 标 题 :Reaction and dissolving medium for peptides and synthesis method using this medium 发明人:GALVEZ MARIE; MAURICE MARIE-FRANCE 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a reaction and dissolving medium for the synthesis of peptides. This reaction and dissolving medium for peptide synthesis and/or purification comprises a diluent A chosen from a group of water-immiscible solvents and a phenol B. By employing this reaction and dissolving medium, peptides can be synthesized which are useful as medicaments, vaccines, agro-foodstuff products or plant protection products.
专利号:WO-2022127920-A1 优先权日:2020-12-18 标 题:Preparation method for and intermediate of 5'-nucleoside prodrug 发明人:SHEN JINGSHAN; HU TIANWEN; XIE YUANCHAO; ZHU FUQIANG 权利人:TOPHARMAN SHANGHAI CO LTD 摘要:Provided in the present invention are a preparation method for and an intermediate of a 5'-nucleoside prodrug. Specifically, provided in the present invention is a method for preparing a compound of formula VI. The method comprises the steps of: (a) reacting a compound of formula I and a compound of formula II to obtain a compound of formula III; (b) reacting the compound of formula III and reagent M to obtain a compound of formula IV; (c) reacting the compound of formula IV in the presence of reagent N to obtain a compound of formula V; and (d) reacting the compound of formula V with reagent O to obtain a compound of formula VI. The preparation method provided by the present invention has the advantages of having low costs, high yield, good product purity and the like, and is capable of achieving the efficient synthesis of 5'-nucleoside prodrugs.
专利号:US-8748604-B2 优先权日:2010-03-04 标 题 :Process for stereoselective synthesis of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine 发明人:KSHIRSAGAR PRAKASH BHIMAJI; BHOGE SATISH MANOHAR; RICHHARIYA SANTOSH; SINGH KAPTAN 权利人:KSHIRSAGAR PRAKASH BHIMAJI; BHOGE SATISH MANOHAR; RICHHARIYA SANTOSH; SINGH KAPTAN; RANBAXY LAB LTD 摘要:The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.
摘要:Simon, R. C.; Busto, E.; Fischereder, E.-M.; Fuchs, C. S.; Pressnitz, D.; Richter, N.; Kroutil, W., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 397. 摘要:Diéguez, M.; Bäckvall, J.-E.; Pàmies, O., Science of Synthesis, (2019) , 194. 摘要:Adriaensen, K.; De Vos, D., Science of Synthesis, (2022) , 162.