专利号:US-11661406-B2 优先权日:2018-08-13 标 题 :Method for producing intermediate useful for synthesis of SGLT inhibitor 发明人:LI QING RI; YOON HEE KYOON 权利人:DAEWOONG PHARMACEUTICAL CO LTD 摘要:A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.
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-11247977-B2 优先权日:2018-06-22 标题 :Compound and use thereof in synthesis of brivaracetam intermediate and crude drug 发明人:FENG YAN; WANG RUYONG; YE YIZHANG; ZHANG FENGSEN; GONG XUAN; WANG ZHONGHONG; KANG XINSHAN 权利人:FUJIAN HAIXI PHARMACEUTICALS CO LTD 摘要:The present application provides a compound in formula III, and further provides a use of the compound in the synthesis of a Brivaracetam intermediate and a crude drug, and a synthesis method. A raw material involved in the method of the present application is low in costs and easily available; (R)-4-propyl-dihydrofuran-2-ketone having high optical purity can be prepared; complicated separation and purification steps are avoided; costs are reduced, and the method is more applicable to industrial production.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-2016317682-A1 优先权日:2015-04-30 标题:PREPARATION OF Ag18F AND ITS USE IN THE SYNTHESIS OF PET RADIOTRACERS 发明人:SCOTT PETER J H; BROOKS ALLEN F; ICHIISHI NAOKO; SANFORD MELANIE S 权利人:UNIV MICHIGAN REGENTS; THE REGENTS OFTHE UNIV OF MICHIGAN 摘要:Copper-catalyzed radiofluorination of aryl iodides using Ag 18 F, methods of preparing Ag 18 F, and compounds obtained by copper-catalyzed radiofluorination of aryl iodides using Ag 18 F are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.
专利号:US-11365211-B2 优先权日:2018-02-01 标 题 :Stereoselective synthesis and process for the manufacturing of 2′-deoxynucleosides 发明人:ZHANG LIANHAO; VISHNUVAJJALA BABURAO; MORRIS JOEL; BAHDE ROBERT; DENYSENKO SERGIY M; LOPEZ OMAR DIEGO; WISHKA DONN GREGORY 权利人:THE USA AS REPRESENTED BY THE SEC DEP OF HEALTH AND HUMAN SERVICES; ALCHEM LABORATORIES CORP; US HEALTH 摘要:Methods for stereoselective synthesis and manufacturing of 2′-deoxynucleosides, such as 2′-ribonucleosides, are disclosed. In some embodiments, the 2′-deoxynucleoside is a β-anomer of a 2′-deoxynucleoside having a 3′ α hydroxyl, 4′ β hydroxymethyl configuration. Nonlimiting examples of compounds prepared by the disclosed methods include 4′-thio-2′-deoxycytidine (T-dCyd) and 5-aza-4′-thio-2′-deoxycytidine (5-aza-T-dCyd; aza-T-dCyd; aza-T-dC).
摘要:Oishi, M.; Takikawa, H., Science of Synthesis Knowledge Updates, (2010) 4, 104. 摘要:Selt, M.; Waldvogel, S. R., Science of Synthesis: Special Topics, (2021) 1, 270. 摘要:Yoshida, T.; Tobisu, M., Science of Synthesis: Special Topics, (2022) 1, 606. 摘要:Fogel, M. S.; Shellnutt, Z. S.; Koide, K., Science of Synthesis: Dearomatizations, (2026) . 摘要:Crousse, B., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 19.