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1. 发明授权

US06559312B2 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：US06559312B2
公开(公告)日：2003-05-06
申请号：US09731654
申请日：2000-12-08
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 of 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0或1的整数; 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。

2. 发明授权

US06552200B2 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：US06552200B2
公开(公告)日：2003-04-22
申请号：US09725259
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： 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 R1represented 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，n为整数0的第二个键。

3. 发明授权

US06479663B2 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：US06479663B2
公开(公告)日：2002-11-12
申请号：US09726625
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： 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表示羟基的整数为0的第二个键。

4. 发明授权

US06566526B2 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：US06566526B2
公开(公告)日：2003-05-20
申请号：US09725291
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： 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 to 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 2一起形成带有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0至1的整数; 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。

5. 发明授权

US06548675B2 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：US06548675B2
公开(公告)日：2003-04-15
申请号：US09729203
申请日：2000-12-05
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 to form a second bond between the carbon atoms R1 and R2 or where R1 represented hydroxy 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R1和R2被取代形成碳原子R1和R2之间的第二个键，或其中R1表示羟基整数0。

6. 发明授权

US06441179B1 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：US06441179B1
公开(公告)日：2002-08-27
申请号：US09818966
申请日：2001-03-28
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。

7. 发明授权

US4211709A Aminopyrrole derivatives 失效
标题翻译：氨基吡咯衍生物
公开(公告)号：US4211709A
公开(公告)日：1980-07-08
申请号：US960386
申请日：1978-11-13
申请人： Giorgio Tarzia , Gianbattista Panzone
发明人： Giorgio Tarzia , Gianbattista Panzone
IPC分类号： C07D207/34 , C07D207/36 , C07D209/40 , C07D207/44
CPC分类号： C07D209/40 , C07D207/34 , C07D207/36
摘要： Pharmacologically-active aminopyrrole derivatives of the formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, benzyl and chlorobenzyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, phenyl and phenyl substituted by a radical selected from methyl, ethyl, methoxy, ethoxy, benzyloxy, fluoro, chloro and bromo;R.sub.2 and R.sub.3 individually represent hydrogen or (C.sub.1-4)alkyl or, taken together, represent an isopropylidene, a benzylidene or a chlorobenzylidene radical;R.sub.4 is selected from (C.sub.2-4)alkanoyl; carbo(C.sub.1-3)alkoxy; benzoyl, benzoyl substituted by a radical selected from chloro, methoxy or ethoxy; carbamoyl, methylcarbamoyl and phenyl carbamoyl;R.sub.5 is selected from hydrogen, (C.sub.1-4)alkyl, carbo(C.sub.1-3)alkoxy, carbomethoxymethyl, carbethoxymethyl, trifluoromethyl and carbamoyl, with the proviso that when R is hydrogen, R.sub.1 and R.sub.5 are methyl and R.sub.4 is carbethoxy, and R.sub.2 and R.sub.3 cannot simultaneously represent hydrogen;and a salt thereof with a pharmaceutically-acceptable acid.The compounds have anti-inflammatory and CNS-depressant utility. They are also useful as analgesics and antipyretics and display a very low degree of anti-ulcerogenic activity.
摘要翻译：式（Ia）的药理学活性氨基吡咯衍生物，其中：R选自氢，（C 1-4）烷基，苄基和氯苄基; R 1选自氢，（C 1-4）烷基，苯基和被选自甲基，乙基，甲氧基，乙氧基，苄氧基，氟，氯和溴的基团取代的苯基; R2和R3分别表示氢或（C1-4）烷基，或者一起表示异亚丙基，亚苄基或氯亚苄基; R4选自（C2-4）烷酰基; 碳（C 1-3）烷氧基; 苯甲酰基，被选自氯，甲氧基或乙氧基的基团取代的苯甲酰基; 氨基甲酰基，甲基氨基甲酰基和苯基氨基甲酰基; R 5选自氢，（C 1-4）烷基，碳（C 1-3）烷氧基，甲酯基甲基，乙氧羰基甲基，三氟甲基和氨基甲酰基，条件是当R为氢时，R 1和R 5为甲基，R 4为乙氧羰基，而R3不能同时代表氢; 及其与药学上可接受的酸的盐。该化合物具有抗炎和CNS抑制作用。它们也可用作镇痛药和解热药，并显示非常低程度的抗溃疡活性。

8. 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。

9. 发明授权

US5750509A Amide derivatives of antibiotic A 40926 失效
标题翻译：抗生素A 40926的酰胺衍生物
公开(公告)号：US5750509A
公开(公告)日：1998-05-12
申请号：US640681
申请日：1996-04-30
申请人： Adriano Malabarba , Romeo Ciabatti , Gianbattista Panzone , Alessandra Maria Marazzi
发明人： Adriano Malabarba , Romeo Ciabatti , Gianbattista Panzone , Alessandra Maria Marazzi
IPC分类号： A61K38/00 , C07K9/00 , A61K38/14 , C07K7/50
CPC分类号： C07K9/008 , A61K38/00 , Y10S930/19
摘要： The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C.sub.1 -C.sub.4) alkoxy-carbonyl, aminocarbonyl, (C.sub.1 -C.sub.4) alkylaminocarbonyl, di (C.sub.4 -C.sub.4)alkylaminocarbonyl or hydroxymethyl substituent on the N-acylaminoglucuronyl moiety and a hydroxy or a polyamine substituent in position 63 of the molecule. The compounds of the invention show high in vitro activity against glycopeptide resistant Enterococci and Staphylococci.
摘要翻译：本发明涉及新型抗菌素A40926衍生物，其特征在于在N-酰氨基葡萄糖醛酸基上具有羧基，（C 1 -C 4）烷氧羰基，氨基羰基，（C 1 -C 4）烷基氨基羰基，二（C 4 -C 4）烷基氨基羰基或羟甲基取代基部分和位于分子63位的羟基或多胺取代基。本发明的化合物显示出对耐糖耐肠球菌和葡萄球菌的高体外活性。

10. 发明授权

US5378837A Process for preparing 2'-(diethylamino)rifamycin P (P/DEA) 失效
标题翻译：制备2' - （二乙基氨基）利福霉素P（P / DEA）
公开(公告)号：US5378837A
公开(公告)日：1995-01-03
申请号：US134515
申请日：1993-10-08
申请人： Gianbattista Panzone , Anacleto Gianantonio
发明人： Gianbattista Panzone , Anacleto Gianantonio
IPC分类号： A61K31/425 , A61K31/429 , A61P31/04 , A61P31/06 , A61P31/12 , C07D513/18 , A61K31/395
CPC分类号： C07D513/18
摘要： The present invention relates to a new one-pot process for preparing 2'-(diethylamino)rifamycin P and its 25-desacetyl derivative which consists in cyclizing 3-bromorifamycin S or its 25-desacetyl derivative, dissolved in dimethylformamide, with 1,1-diethylthiourea and reducing, without isolation, the obtained 1,2-quinonimine intermediate with a mild reducing agent.
摘要翻译：本发明涉及一种制备2' - （二乙基氨基）利福霉素P及其25-去乙酰基衍生物的新的一锅法，该方法包括将溶解在二甲基甲酰胺中的3-溴霉素S或其25-脱乙酰基衍生物环化，并将所得1,2-醌亚胺中间体用温和还原剂还原，不分离。

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