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    METHODS FOR PRODUCING PHENYLALANINE DERIVATIVES HAVING A QUINAZOLINEDIONE SKELETON AND INTERMEDIATES FOR PRODUCTION THEREOF
    1.
    发明申请
    METHODS FOR PRODUCING PHENYLALANINE DERIVATIVES HAVING A QUINAZOLINEDIONE SKELETON AND INTERMEDIATES FOR PRODUCTION THEREOF 有权
    用于生产具有四氮唑烷酮的苯乙烯胺衍生物的方法及其生产中间体

    公开(公告)号：US20100204505A1

    公开(公告)日：2010-08-12

    申请号：US12766178

    申请日：2010-04-23

    申请人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    发明人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    IPC分类号： C07C229/52

    CPC分类号： C07D239/96 ,  C07C233/87

    摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译： 本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤， 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基 等等。

    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof
    2.
    发明授权
    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
    具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体

    公开(公告)号：US08318975B2

    公开(公告)日：2012-11-27

    申请号：US12766178

    申请日：2010-04-23

    申请人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    发明人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    IPC分类号： C07C63/04

    CPC分类号： C07D239/96 ,  C07C233/87

    摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译： 本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤， 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基 等等。

    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof
    3.
    发明授权
    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
    具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体

    公开(公告)号：US07737274B2

    公开(公告)日：2010-06-15

    申请号：US11207751

    申请日：2005-08-22

    申请人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    发明人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    IPC分类号： A61K31/517 ,  C07D239/80 ,  C07D239/88 ,  C07C61/08 ,  C07C63/06 ,  C07C229/56

    CPC分类号： C07D239/96 ,  C07C233/87

    摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译： 本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤， 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基 等等。

    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof
    4.
    发明申请
    Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
    具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体

    公开(公告)号：US20060009476A1

    公开(公告)日：2006-01-12

    申请号：US11207751

    申请日：2005-08-22

    申请人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    发明人： Noriyasu Kataoka ,  Akinori Tatara ,  Masanobu Yatagai ,  Junko Yamanaka

    IPC分类号： A61K31/517 ,  C07D239/91

    CPC分类号： C07D239/96 ,  C07C233/87

    摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.

    摘要翻译： 本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤， 和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。 该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。 在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基 等等。

    Process for preparing antifungal V-28-3M
    5.
    发明授权
    Process for preparing antifungal V-28-3M 失效
    抗真菌V-28-3M的制备方法

    公开(公告)号：US06346610B1

    公开(公告)日：2002-02-12

    申请号：US09445240

    申请日：1999-12-03

    申请人： Noriyasu Kataoka ,  Kenzo Tanaka ,  Masanobu Yatagai

    发明人： Noriyasu Kataoka ,  Kenzo Tanaka ,  Masanobu Yatagai

    IPC分类号： C07M100

    CPC分类号： C07H17/08 ,  Y02P20/55

    摘要： An industrially suitable process for preparing V-28-3M useful as an antimycotic agent by conducting methyl esterification of V-28-3 efficiently. V-28-2 is efficiently converted into V-28-3M by protecting the amino group of the amino sugar of V-28-3 with an appropriate protecting group, subjecting the carboxyl group of V-28-3 to methyl esterification with methyl methanesulfonate or methyl p-toluenesulfonate in the presence of a base, and deprotecting the N-protected intermediate.

    摘要翻译： 通过有效地进行V-28-3的甲基酯化，可以制备适用于抗真菌剂的V-28-3M的工业上合适的方法。 通过用合适的保护基保护V-28-3的氨基糖的氨基，V-28-2的羧基被甲基酯化，V-28-2被有效地转化成V-28-3M 甲磺酸酯或对甲苯磺酸甲酯在碱的存在下脱保护，并保护N-保护的中间体。

    Method of producing optically active cyclopropane derivatives
    6.
    发明授权
    Method of producing optically active cyclopropane derivatives 失效
    光学活性环丙烷衍生物的制备方法

    公开(公告)号：US5900492A

    公开(公告)日：1999-05-04

    申请号：US982458

    申请日：1997-12-02

    申请人： Katsutoshi Sakata ,  Takashi Tsuji ,  Noriyasu Kataoka ,  Masanobu Yatagai

    发明人： Katsutoshi Sakata ,  Takashi Tsuji ,  Noriyasu Kataoka ,  Masanobu Yatagai

    IPC分类号： C07C69/757 ,  C07C211/27 ,  C07D307/93 ,  C07D307/00

    CPC分类号： C07C69/757 ,  C07C211/27 ,  C07D307/93

    摘要： A method for resolving optically impure 3-oxa-2-oxobicyclo�3.1.0!hexane-1-carboxylic acid esters. A method is provided for producing a 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid.N-benzyl-.alpha.-phenylethylamine diastereomer salt. An enantiomer of N-benzyl-.alpha.-phenylethylamine is reacted with a 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid to produce a precipitate that is enriched in one diastereomer of the salt. After isolating the optically active salt, the N-benzyl-.alpha.-phenylethylamine may be separated to produce the corresponding 1-alkoxycarbonyl-2-hydroxymethylcyclopropane-1-carboxylic acid. Under acidic conditions, the carboxylic acid and hydroxyl groups undergo ring closure to afford the optically active 3-oxa-2-oxobicyclo�3.1.0!hexane-1-carboxylic acid ester.

    摘要翻译： 一种拆分光学上不纯的3-氧杂-2-氧代双环[3.1.0]己烷-1-羧酸酯的方法。 提供了制备1-烷氧基羰基-2-羟甲基环丙烷-1-羧酸N-苄基-α-苯乙胺非对映体盐的方法。 N-苄基-α-苯乙基胺的对映异构体与1-烷氧基羰基-2-羟甲基环丙烷-1-羧酸反应，产生富含一种盐的非对映异构体的沉淀物。 分离光学活性盐后，可以分离N-苄基-α-苯乙胺，生成相应的1-烷氧基羰基-2-羟甲基环丙烷-1-羧酸。 在酸性条件下，羧酸和羟基发生闭环，得到光学活性3-氧杂-2-氧代双环[3.1.0]己烷-1-羧酸酯。

    Process for isolating 2-amino-6-chloro-9-[(1'S,2'R)-1'2'-bis(hydroxymethyl)-cyclopropane-1'-YL]methylpurine and an optical isomer thereof
    9.
    发明授权
    Process for isolating 2-amino-6-chloro-9-[(1'S,2'R)-1'2'-bis(hydroxymethyl)-cyclopropane-1'-YL]methylpurine and an optical isomer thereof 有权
    分离2-氨基-6-氯-9 - [（1'S，2'R）-1'2'-双（羟甲基） - 环丙烷-1'-YL]甲基嘌呤及其旋光异构体的方法

    公开(公告)号：US06172224B2

    公开(公告)日：2001-01-09

    申请号：US09263999

    申请日：1999-03-08

    申请人： Noriyasu Kataoka ,  Toshihiro Matsuzawa ,  Masanobu Yatagai

    发明人： Noriyasu Kataoka ,  Toshihiro Matsuzawa ,  Masanobu Yatagai

    IPC分类号： C07D47332

    CPC分类号： C07D473/00

    摘要： A process for purifying 2-amino-6-chloro-9-[(1′S,2′R)-1′,2′-bis(hydroxymethyl) cycdopropane-1′-yl]methylpurine represented by the following formula (5) comprises the step of selectively isolating 2-amino-6-chloro-9-[(1′S,2′R)-1′,2′-bis(hydroxymethyl) cyclopropane-1′-yl]methylpurine from a mixture of 2-amino-6-chloro-9-[(1′S,2′R)-1′,2′-bis(hydroxymethyl)cyclopropane-1′-yl]methylpurine and 2-amino-6-chloro-7-[(1′S,2′R)-1′,2′-bis(hydroxymethyl)cyclopropane-1′-yl]methylpurine represented by the following formula (6) by the crystallization. This process has a satisfactory medicinal quality on an industrial scale without necessitating complicated operations such as chromatographic purification.

    摘要翻译： 用于纯化由下式（5）表示的2-氨基-6-氯-9 - [（1'S，2'R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤的方法包括 从2-氨基-6-氯-9 - [（1'S，2'R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤的2-氨基-6- 6-氯-9 - [（1'S，2'R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤和2-氨基-6-氯-7 - [（1'S，2' R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤通过结晶表示。 该方法在工业规模上具有令人满意的药用质量，而不需要色谱纯化等复杂操作。