CAS: 135540-11-3; 1-(Chloro(Pyrrolidin-1-yl)Methylene)Pyrrolidin-1-Ium Hexafluorophosphate(V)

该化合物是一种高反应性试剂,通常用于联和其他有机合成应用,其主要优点包括作为活性剂的高反应性,促进以最小的种族化方式高效的氨化联结形成.六氟磷基反作用会提高有机溶剂的溶性,改善反应同质性.该化合物在无水条件下的稳定性能确保敏感合成工艺的一贯性能.其结构设计能促进箱式酸的选择性活化,使其对复杂的化和制药合成具有价值.在自动的固相聚(SPS)中,它能提供可靠的产量和与一系列保护组的兼容性.

结构式图片

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115007-14-2 164298-25-3 1204324-19-5

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合成工艺路线路线简述

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    专利信息


    专利号:US-2022233673-A1
    优先权日:2019-06-04
    标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
    发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
    权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
    摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

    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-2025129050-A1
    优先权日:2022-01-26
    标 题 :Synthesis of a kif18a inhibitor
    发明人:CAILLE SEBASTIEN; GREENE DANIEL GERARD; CORBETT MICHAEL THOMAS; WEI CAROLYN
    权利人:AMGEN INC
    摘要:The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).

    专利号:WO-2023146973-A1
    优先权日:2022-01-26
    标题 :Synthesis of a kif18a inhibitor

    专利号:EP-4469437-A1
    优先权日:2022-01-26
    标 题 :Synthesis of a kif18a inhibitor

    专利号:CN-118922406-A
    优先权日:2022-01-26
    标题 :Synthesis of KIF18A inhibitors
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    合成参考文献


    参考文献:10.1134/s1068162021020291
    摘要:Zhukov SA, Pyshnyi DV, Kupryushkin MS. Synthesis of Novel Representatives of Phosphoryl Guanidine Oligonucleotides. Russian Journal of Bioorganic Chemistry. 2021 Mar;47(2):380–9. doi: 10.1134/s1068162021020291.
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