中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

775 records (took 0.098 seconds)

    Fluorination method
    174.
    发明授权
    Fluorination method 有权

    公开(公告)号：US10287220B2

    公开(公告)日：2019-05-14

    申请号：US15127599

    申请日：2015-03-20

    Applicant: Oxford University Innovation Limited

    Inventor： Veronique Gouverneur ,  Matthew Tredwell ,  Sean Preshlock

    IPC: C07D295/16 ,  C07B59/00 ,  C07F5/04 ,  C07C17/361 ,  C07C37/62 ,  C07C41/22 ,  C07C45/65 ,  C07C67/317 ,  C07C201/12 ,  C07C209/74 ,  C07C231/12 ,  C07C253/30 ,  C07C303/40 ,  C07D209/08 ,  C07D215/18 ,  C07D277/30 ,  C07D295/073 ,  C07F5/02

    Abstract: The present invention relates to a process for producing an organic compound comprising an 18F atom. The compounds comprising an 18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridized carbon atom, with (i) 18F— and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp2 hybridized carbon atom, in a process for producing an organic compound comprising an 18F atom, which process comprises treating the organoboron compound with (i)18F— and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PGA is independently H or an alcohol protecting group; PGB is H or a carboxylic acid protecting group; each PGC is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.

    PROCESS FOR THE PREPARATION OF IOPAMIDOL
    175.
    发明申请
    PROCESS FOR THE PREPARATION OF IOPAMIDOL 审中-公开

    公开(公告)号：US20190077745A1

    公开(公告)日：2019-03-14

    申请号：US16052695

    申请日：2018-08-02

    Applicant: BRACCO IMAGING S.P.A.

    Inventor： Elisa BATTISTINI ,  Federica BUONSANTI ,  Daniela IMPERIO ,  Luciano LATTUADA ,  Roberta NAPOLITANO

    IPC: C07C231/14 ,  C07C231/02 ,  C07F5/04 ,  C07F5/05 ,  C07F5/02 ,  C07C201/12 ,  C07C227/04 ,  C07C231/12 ,  C07C237/46

    Abstract: The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N-(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness.

Patent Agency Ranking