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    Method for Producing Sodium Fosphenytoin
    4.
    发明申请
    Method for Producing Sodium Fosphenytoin 审中-公开
    生产苯丙酸钠的方法

    公开(公告)号：US20070219378A1

    公开(公告)日：2007-09-20

    申请号：US10587189

    申请日：2004-02-05

    Applicant: Hartmut Zinser ,  Guisep Derungs

    Inventor： Hartmut Zinser ,  Guisep Derungs

    IPC: C07D233/00

    CPC classification number: C07F9/6506

    Abstract: Sodium fosphenytoin, 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione disodium salt, a known anticonvulsive, antiepileptic and antiarrhythmic, can be prepared by reacting 3-hydroxymethyl-5,5-diphenylimidazoline-2,4-dione with a phosphorous acid diester or triester activated by an oxidizing agent, whose ester groups can be selectively cleaved from the reaction product, cleaving the ester groups from the resulting phosphoric acid diester 2,5-dioxo-4,4-diphenyl-imidazolidin-1-ylmethyl ester and converting the resulting 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione to its disodium salt. The oxidizing agent is advantageously a halogenating agent such as elemental bromine or N-bromosuccinimide, and the phosphorous acid ester used is advantageously dibenzyl phosphite. Of particular importance—even taken on its own—is the fact that a phosphoric acid diester 2,5-dioxo-4,4-diphenylimidazolidin-1-ylmethyl ester, whose phosphoric acid diester structural element can be selectively cleaved, can be converted to 5,5-diphenyl-3-[(phosphonooxy)methyl]imidazolidine-2,4-dione and the latter converted to its disodium salt in a single operation.

    Abstract translation: 已知的抗惊厥，抗癫痫和抗心律失常药的5-苯基苯并噻吩钠，5,5-二苯基-3 - [（膦酰氧基）甲基]咪唑烷-2,4-二酮二钠盐可以通过3-羟甲基-5,5-二苯基咪唑啉-2 具有通过氧化剂活化的亚磷酸二酯或三酯的2,4-二酮，其酯基可以从反应产物中选择性地裂解，从所得的磷酸二酯2,5-二氧代-4,4-二酮中切割酯基， 并将所得的5,5-二苯基-3 - [（膦酰氧基）甲基]咪唑烷-2,4-二酮转化成其二钠盐。 氧化剂有利地是卤化剂如元素溴或N-溴代琥珀酰亚胺，并且所用的亚磷酸酯有利地是亚磷酸二苄酯。 特别重要的是甚至独自考虑的事实是，其磷酸二酯结构单元可以选择性地裂解的磷酸二酯2,5-二氧代-4,4-二苯基咪唑烷-1-基甲酯可以转化为 5,5-二苯基-3 - [（膦酰氧基）甲基]咪唑烷-2,4-二酮，后者在一次操作中转化成其二钠盐。

    Process for the preparation of (3r,3as,6ar)-hexahydrofuro [2,3-b] furan-3-yl (1s,2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate
    6.
    发明申请
    Process for the preparation of (3r,3as,6ar)-hexahydrofuro [2,3-b] furan-3-yl (1s,2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate 有权
    制备（3r，3as，6ar）六氢呋喃并[2,3-b]呋喃-3-基（1s，2r）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1 苄基-2-羟丙基氨基甲酸酯

    公开(公告)号：US20070060642A1

    公开(公告)日：2007-03-15

    申请号：US10596732

    申请日：2004-12-23

    Applicant: Nicolaas Martha Felix Goyvaerts ,  Piet Wigerinck ,  Hartmut Zinser ,  Birgit Ebert

    Inventor： Nicolaas Martha Felix Goyvaerts ,  Piet Wigerinck ,  Hartmut Zinser ,  Birgit Ebert

    IPC: A61K31/343 ,  C07D493/02

    CPC classification number: C07D493/02 ,  C07D493/04

    Abstract: The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate as well as intermediates for use in said process. More in particular the invention relates to processes for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate which make use of 4-amino-N-((2R,3S)-3-amino-2-hydroxy-4-phenylbutyl)-N-(isobutyl)benzene sulfonamide intermediate, and to processes amenable to industrial scaling up. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl (1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as HIV protease inhibitors.

    Abstract translation: 本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸酯以及用于所述方法的中间体。 更具体地，本发明涉及制备（3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基] 使用4-氨基-N - （（2R，3S）-3-氨基-2-羟基-4-苯基丁基）-N-（异丁基）苯磺酰胺的（异丁基）氨基] -1-苄基-2-羟基丙基氨基甲酸叔丁酯 中间和适用于工业规模化的流程。 （3R，3aS，6aR） - 六氢呋喃并[2,3-b]呋喃-3-基（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2- 羟丙基氨基甲酸酯特别可用作HIV蛋白酶抑制剂。

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