PROCESS SIMPLIFICATION FOR PRECURSOR COMPOUND
    65.
    发明申请
    PROCESS SIMPLIFICATION FOR PRECURSOR COMPOUND 有权
    前体化合物的工艺简化

    公开(公告)号:US20130274507A1

    公开(公告)日:2013-10-17

    申请号:US13994781

    申请日:2011-12-19

    IPC分类号: C07B59/00 C07C227/18

    摘要: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET tracer.

    摘要翻译: 本发明涉及一种用于制备放射性药物前体的方法,特别是用作生产用于体内成像方法如正电子发射断层摄影(PET)的放射性标记氨基酸的前体的保护的氨基酸衍生物。 特别地,本发明涉及制备可用于制备[18 F] -1-氨基-3-氟环丁烷羧酸([18 F] FACBC))PET示踪剂的前体的方法。

    Process for the preparation of anagrelide and analogues
    67.
    发明授权
    Process for the preparation of anagrelide and analogues 有权
    制备阿那格雷和类似物的方法

    公开(公告)号:US08530651B2

    公开(公告)日:2013-09-10

    申请号:US13132001

    申请日:2009-11-30

    申请人: Bernard Golding

    发明人: Bernard Golding

    IPC分类号: C07D487/04

    摘要: The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.

    摘要翻译: 本发明涉及可用于治疗的喹唑啉化合物的新方法。 更具体地,通过本发明的方法生产的化合物可用于治疗许多心血管疾病。 本发明的方法以清洁和有效的方式提供了6,7-二氯-1,5-二氢咪唑并[2,1-b]喹唑啉2(3H) - 酮,更通常称为阿那格雷及其类似物。

    Process for Preparing Crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic Acid and Use for Production of Primovist®
    69.
    发明申请
    Process for Preparing Crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic Acid and Use for Production of Primovist® 审中-公开
    制备结晶3,6,9-三氮杂-3,6,9-三(羧甲基)-4-(4-乙氧基苄基)十一烷二酸的方法和用于生产Primovist®

    公开(公告)号:US20130158241A1

    公开(公告)日:2013-06-20

    申请号:US13703579

    申请日:2011-06-06

    IPC分类号: C07C227/18 C07C229/26

    摘要: The invention relates to a method for producing crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I by saponifying 3,6,9-triaza-3,6,9-tris(tert-butoxycarbonylmethyl)-4-(4-ethoxybenzyl)-undecanedioic acid di-tert-butyl ester of the formula II in an aqueous alkali metal hydroxide solution and using 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I for producing the gadolinium complex of 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid [(Gd-EOB-DTPA)=Primovist®].

    摘要翻译: 本发明涉及通过皂化3,6,9-三氮杂的方法制备式I的结晶3,6,9-三氮杂-3,6,9-三(羧甲基)-4-(4-乙氧基苄基)十一烷二酸 -3,6,9-三(叔丁氧基羰基甲基)-4-(4-乙氧基苄基) - 十二烷二酸二叔丁酯在碱金属氢氧化物水溶液中,并使用3,6,9-三氮杂 具有式I的-3,6,9-三(羧甲基)-4-(4-乙氧基苄基)十一烷二酸,用于制备3,6,9-三氮杂-3,6,9-三(羧甲基) - 4-(4-乙氧基苄基)十一烷二酸[(Gd-EOB-DTPA)= Primovist]。