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1. 发明授权

US4237304A Oxazolinium salts and method of preparation 失效
标题翻译： 唑啉盐及其制备方法
公开(公告)号：US4237304A
公开(公告)日：1980-12-02
申请号：US955039
申请日：1978-10-26
申请人： William Dowd , Richard C. Krauss , Edward R. Freiter
发明人： William Dowd , Richard C. Krauss , Edward R. Freiter
IPC分类号： C07D263/10 , C07D263/12 , C07D263/14
CPC分类号： C07D263/10
摘要： 1-Aryl-1-hydroxy-2-methylaminopropanes are rearranged from the erythro isomer to the threo isomer by the process of (1) forming the O,N-diacyl derivative of the arylpropanolamine; (2) reacting the product of step (1) with an anhydrous or substantially anhydrous protic acid (thereby forming a novel oxazolinium salt); and (3) reacting the oxazolinium salt from step (2) with an aqueous protic acid. The threo isomer of the arylpropanolamine is thus produced as an amine/acid salt. This salt can be further purified, if desired, by neutralizing the acid/amine salt with caustic isolating the free amine and reprotonating the free base in isopropanol with, for example, anhydrous HCl. This process is particularly applicable to manufacture of d-pseudoephedrine from 1-ephedrine.
摘要翻译：通过（1）形成芳基丙醇胺的O，N-二酰基衍生物的方法将1-芳基-1-羟基-2-甲基氨基丙烷从红异构体重排为苏式异构体; （2）使步骤（1）的产物与无水或基本上无水的质子酸（从而形成新的恶唑啉盐）反应; 和（3）使来自步骤（2）的恶唑啉盐与水性质子酸反应。因此，芳基丙醇胺的苏式异构体以胺/酸盐的形式制备。如果需要，该盐可以通过用分离游离胺的苛性碱中和酸/胺盐进一步纯化，并用例如无水HCl将异丙醇中的游离碱重新分配。该方法特别适用于从1-麻黄素制备d-伪麻黄素。

2. 发明授权

US06348597B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06348597B2
公开(公告)日：2002-02-19
申请号：US09824788
申请日：2001-04-04
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 和其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

3. 发明授权

US06777555B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06777555B2
公开(公告)日：2004-08-17
申请号：US10364641
申请日：2003-02-12
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, n is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，n是整数0。

4. 发明授权

US6147216A Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US6147216A
公开(公告)日：2000-11-14
申请号：US458747
申请日：1995-06-02
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07C45/46 , C07C45/63 , C07C45/65 , C07C45/67 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07D211/22 , C07D295/185 , C07D401/06 , C07D401/10 , C07D211/14
CPC分类号： C07D295/185 , C07C235/78 , C07C255/16 , C07C259/06 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07D211/22 , C07D401/06 , C07D401/10 , C07C2101/02
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula ##STR1## wherein W represents --C(.dbd.O)-- or --CH(OH)--;R.sub.1 represents hydrogen or hydroxy;R.sub.2 represents hydrogen;R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;n is an integer of from 1 to 5;m is an integer 0 or 1;R.sub.3 is --COOH or --COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R.sub.1 and R.sub.2 are ta to form a second bond between the carbon R.sub.1 and R.sub.2 or where R.sub.1 represented hydroxy integer 0.
摘要翻译：本发明涉及可用于制备下式其中W代表-C（= O） - 或-CH（OH） - 的某些抗组氨酸哌啶衍生物的新中间体和方法; R1代表氢或羟基; R2表示氢; R1和R2一起形成带有R1和R2的碳原子之间的第二个键; n为1〜5的整数， m为整数0或1; R3是-COOH或-COO烷基，其中烷基部分具有1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 以及其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2为ta以在碳R 1和R 2之间形成第二个键，或其中R 1表示羟基整数0。

5. 发明授权

US4410701A Process for making pyridyloxyphenol compounds 失效
标题翻译：制备吡啶氧基苯酚化合物的方法
公开(公告)号：US4410701A
公开(公告)日：1983-10-18
申请号：US373386
申请日：1982-04-30
申请人： Richard C. Krauss
发明人： Richard C. Krauss
IPC分类号： C07D213/64 , C07D213/643
CPC分类号： C07D213/643
摘要： Process for making pyridyloxyphenol by reacting under essentially anhydrous conditions in the absence of oxygen and in a polar aprotic solvent, a 2-halopyridine with hydroquinone which has been from 75 to 100 percent neutralized to the sodium or potassium salt.
摘要翻译：通过在基本上无水条件下在不存在氧的情况下和极性非质子溶剂中反应制备吡啶氧基苯酚的方法，其中氢醌的2-卤代吡啶已经从75至100％中和至钠盐或钾盐。

6. 发明授权

US06555689B2 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06555689B2
公开(公告)日：2003-04-29
申请号：US09726580
申请日：2000-12-01
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21122
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，为直链或支链; A为氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

7. 发明授权

US06340761B1 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06340761B1
公开(公告)日：2002-01-22
申请号：US09725298
申请日：2000-11-29
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，并且是直链或支链的，每个A是氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

8. 发明授权

US06242606B1 Intermediates useful for the preparation of antihistaminic piperidine derivatives 失效
标题翻译：用于制备抗组胺型哌啶衍生物的中间体
公开(公告)号：US06242606B1
公开(公告)日：2001-06-05
申请号：US08275685
申请日：1994-07-14
申请人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
发明人： Richard C. Krauss , Robert M. Strom , Carey L. Scortichini , William J. Kruper , Richard A. Wolf , Weishi W. Wu , Albert A. Carr , David A. Hay , Duane E. Rudisill , Gianbattista Panzone
IPC分类号： C07D21114
CPC分类号： C07D295/185 , C07C33/46 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/673 , C07C49/792 , C07C49/798 , C07C49/80 , C07C49/813 , C07C49/82 , C07C49/825 , C07C49/83 , C07C49/835 , C07C49/86 , C07C59/86 , C07C59/88 , C07C69/007 , C07C69/738 , C07C235/78 , C07C255/16 , C07C259/06 , C07C2601/02 , C07D211/22 , C07D401/06 , C07D401/10
摘要： The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
摘要翻译：本发明涉及一种新的中间体和方法，其可用于制备W代表-C（= O） - 或-CH（OH） - 的某些抗组胺型哌啶衍生物; R 1表示氢或羟基; R 2表示氢 R 1和R 2一起形成在具有R 1和R 2的碳原子之间的第二个键; n是1至5的整数; m是整数0或1; R 3是-COOH或-COO烷基，其中烷基部分具有 1至6个碳原子，为直链或支链; A为氢或羟基; 其药学上可接受的盐和单独的光学异构体，条件是其中R 1和R 2一起形成在具有R 1和R 2的碳原子之间或其中R 1表示羟基的第二个键，m是整数0。

9. 发明授权

US5008396A Process for the preparation of 5-amino-3-chlorosulfonyl-1,2,4-triazole 失效
标题翻译： 5-氨基-3-氯磺酰基-1,2,4-三唑的制备方法
公开(公告)号：US5008396A
公开(公告)日：1991-04-16
申请号：US432289
申请日：1989-11-06
申请人： Richard C. Krauss
发明人： Richard C. Krauss
IPC分类号： C07D249/12 , C07D249/14
CPC分类号： C07D249/14
摘要： 5-Amino-3-chlorosulfonyl-1,2,4-triazole is prepared by the chlor-oxidation of 5-amino-3-mercapto-1,2,4-triazole. The process is characterized by the preformation of disulfide from the mercaptan prior to treatment with chlorine. The 5-amino-3-chlorosulfonyl-1,2,4-triazole reaction mixture can be directly reacted with substituted anilines to prepare N-(3-(((aryl)amino)sulfonyl)-1H-1,2,4-triazol-5-yl)amines which are useful intermediates for the manufacture of herbicides.

10. 发明授权

US4988812A Aqueous process for the preparation of 5-methyl-n-(aryl)-1,2,4-triazolo(1,5-A)pyrimidine-2-sulfonamides 失效
标题翻译：用于制备5-甲基 - 正 - （芳基）-1,2,4-三唑并（1,5-A）嘧啶-2-磺酰胺的水性方法
公开(公告)号：US4988812A
公开(公告)日：1991-01-29
申请号：US432241
申请日：1989-11-06
申请人： Kay K. Kim , Richard C. Krauss , Jon A. Orvik
发明人： Kay K. Kim , Richard C. Krauss , Jon A. Orvik
IPC分类号： A01N43/90 , C07D249/14 , C07D487/04
CPC分类号： C07D487/04
摘要： 5-Methyl-N-(aryl)-1,2,4-triazolo[1,5-a]-pyrimidine-2-sulfonamides are prepared by the cyclization of N -(3-(((aryl)amino)sulfonyl)-1H-1,2,4-triazol-5-yl)amines with 4-methoxy-3-butene-2-one or its synthetic equivalents in the presence of an aqueous base. By controlling the pH of the condensation between 8.5 and 10.5, by-product formation can be substantially reduced.

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