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    Bile acid salts
    2.
    发明授权
    Bile acid salts 失效
    胆酸盐

    公开(公告)号：US06479681B2

    公开(公告)日：2002-11-12

    申请号：US09934603

    申请日：2001-08-23

    申请人： Marino Brocchetta ,  Chiara Gallotti ,  Massimo Visigalli ,  Pier Lucio Anelli

    发明人： Marino Brocchetta ,  Chiara Gallotti ,  Massimo Visigalli ,  Pier Lucio Anelli

    IPC分类号： C07J4100

    CPC分类号： C07J9/00

    摘要： A process for the preparation of the compounds of general formula (I) in which R1 is H or OH; R2 is H, &agr;-OH, or &bgr;-OH; and R3 is a straight or branched C1-C4 alkyl group or a benzyl group, comprising the reduction of compounds of formula (III) wherein R1, R2 and R3 have the same meanings as in formula I, in the presence of sodium borohydride.

    摘要翻译： 制备通式（I）的化合物的方法，其中R 1为H或OH; R 2为H，α-OH或β-OH; 和R 3是直链或支链C 1 -C 4烷基或苄基，包括在硼氢化钠存在下还原其中R 1，R 2和R 3具有与式I中相同含义的式（III）化合物。

    Process for the preparation of iopamidol and the new intermediated therein
    7.
    发明授权
    Process for the preparation of iopamidol and the new intermediated therein 有权
    制备碘帕醇及其中间体的方法

    公开(公告)号：US07034183B2

    公开(公告)日：2006-04-25

    申请号：US10433389

    申请日：2001-11-29

    申请人： Pier Lucio Anelli ,  Marino Brocchetta ,  Giovanna Lux ,  Enrico Cappelletti

    发明人： Pier Lucio Anelli ,  Marino Brocchetta ,  Giovanna Lux ,  Enrico Cappelletti

    IPC分类号： C07C233/65

    CPC分类号： C07C231/02 ,  C07C237/46

    摘要： A process for the preparation of (S)-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxo-propyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide (iopamidol) starting from 5-amino-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein R1 is a hydrogen atom, a C1÷C4 straight or branched alkoxy group, R2 is hydrogen, a C1÷C4 straight or branched alkoxy group and R3 ?is a C1÷C4 straight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic protections of the hydroxy groups in the carboxamido substituents under acidic conditions, when R is a group of formula A carboxamido hydroxy groups under acidic conditions. The invention also refers to the new intermediates of formula (III) and (IV) wherein —R is a group A.

    摘要翻译： 制备（S）-N，N'-双[2-羟基-1-（羟甲基）乙基] -5 - [（2-羟基-1-氧代 - 丙基）氨基] -2,4， 5-氨基-N，N'-双[2-羟基-1-（羟甲基）乙基] -2,4,6-三碘-1,3-苯二甲酰胺的6-三碘-1,3-苯二甲酰胺（碘帕醇） （II）所述方法包括a）使式（II）化合物与合适的保护剂反应，得到其中R为式A或B的基团的式（III）化合物，其中R 1 >是氢原子，C 1或C 4直链或支链烷氧基，R 2是氢，C 1 直链或支链烷氧基，R 3？是C / C 直链或支链烷基，三氟甲基或三氯甲基; b）通过与（S）-2-（乙酰氧基）丙酰氯反应，酰化式（III）中间体化合物的第5位的氨基，得到其中R如上定义的式（Ⅳ）化合物; 和c）在碱性条件下除去存在于式（Ⅳ）化合物中的所有酰基，在R是式A的基团时，先前在酸性条件下，在甲酰氨基取代基中羟基的环保保护被切割。 在酸性条件下。 本发明还涉及式（III）和（IV）的新中间体，其中-R是基团A.

    Process for the manufacturing of iodinated contrast agents
    8.
    发明授权
    Process for the manufacturing of iodinated contrast agents 失效
    碘化造影剂的制造方法

    公开(公告)号：US5728877A

    公开(公告)日：1998-03-17

    申请号：US685034

    申请日：1996-07-23

    申请人： Pier Lucio Anelli ,  Marino Brocchetta ,  Ornella Gazzotti ,  Fulvio Uggeri

    发明人： Pier Lucio Anelli ,  Marino Brocchetta ,  Ornella Gazzotti ,  Fulvio Uggeri

    IPC分类号： C07C231/12 ,  C07C235/48 ,  C07C237/46 ,  C07C233/65

    CPC分类号： C07C231/12

    摘要： A process for the preparation of compounds of general formula (I) ##STR1## characterized in that the corresponding derivatives of general formula (II) ##STR2## are reacted with the compounds of general formula (III) ##STR3## wherein Z is halogen atom or a reactive residue of a sulfonic acid or a --N.sup.+ (R.sub.9).sub.3 cation wherein R.sub.9 is a (C.sub.1 -C.sub.6) alkyl group and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 R.sub.6 R.sub.7 and R.sub.8 are as herein defined.

    摘要翻译： 制备通式（I）化合物（I）的方法，其特征在于通式（II）的相应衍生物与式（III）的化合物反应：IMAGE （III）其中Z是卤素原子或磺酸或-N +（R9）3阳离子的反应性残基，其中R9是（C1-C6）烷基，R1，R2，R3，R4，R5 R6 R7和 R8如本文所定义。