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-2024092821-A1 优先权日:2020-03-31 标题:Synthesis of oligonucleotides and related compounds 发明人:ZHONG MINGHONG; JIN YI; GALA DINESH; PRHAVC MARIJA 权利人:JANSSEN BIOPHARMA INC 摘要:Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-2012302756-A1 优先权日:2010-02-19 标 题 :Process for synthesis of 2-substituted pyrrolidines and piperadines 发明人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 权利人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 摘要:The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
专利号:WO-2024012791-A1 优先权日:2022-07-11 标题 :Electrochemical synthesis of pyrazolines and pyrazoles 发明人:BÄR ROBIN MAXIMILIAN; FORD MARK JAMES; KALDAS SHERIF JAMES; WALDVOGEL SIEGFRIED; HOFMANN SILJA; LINDEN MARTIN 权利人:BAYER AG 摘要:The present invention relates to an electrochemical process for the synthesis of pyrazolines and pyrazoles of formula (I). The process can be especially used for the synthesis of the herbicide safener mefenpyr-diethyl.
专利号:WO-2023102600-A1 优先权日:2021-12-06 标题:Synthesis of amphiphilic block copolymers and polymeric nanofibers produced therefrom 发明人:ZETTERLUND PER B; ISHIZUKA FUMI; KIM HYUN JIN; CHATANI SHUNSUKE; NIINO HIROSHI 权利人:NEWSOUTH INNOVATIONS PTY LTD 摘要:The present disclosure relates to the field of synthesis of block copolymers, and polymeric nanofibers having a core-shell morphology produced therefrom. The present disclosure relates to the field of synthesis of block copolymers where one block is more hydrophobic than the other block and is a different composition. The disclosure also relates to uses of these polymeric nanofibers in various applications, such as reinforcing a polymeric matrix and for coatings applications.