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1. 发明申请

US20070129573A1 Process for the synthesis of eneamide derivatives 有权
标题翻译：合成烯酰胺衍生物的方法
公开(公告)号：US20070129573A1
公开(公告)日：2007-06-07
申请号：US10583902
申请日：2004-12-22
申请人： Alain Burgos , Blandine Bertrand , Sonia Roussiasse , Jean-Francois Pluvie , Sylvie Blanchet , Juliette Martin , Florence Perrin , Francoise Bourdeau
发明人： Alain Burgos , Blandine Bertrand , Sonia Roussiasse , Jean-Francois Pluvie , Sylvie Blanchet , Juliette Martin , Florence Perrin , Francoise Bourdeau
IPC分类号： C07C233/06
CPC分类号： C07C231/10 , C07C233/06 , C07C2602/08 , C07C2602/10
摘要： A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) where R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)mX wherein R4, m and X are as defined above.
摘要翻译：制备由式（I）表示的烯 - 酰胺衍生物的方法，其中R 1和R 2和R 3独立地为氢原子，烷基，环烷基，环烷基烷基，烷基芳基，芳基，杂环，氰基，烷氧基，芳氧基，羧基，氨基甲酰基，-CONR 5 R 6（其中R 5和R 6独立地为所述被取代的环的烷基，芳基烷基或芳基被取代或不被官能团取代或与R5）或-COOR5基团其中R5是烷基，烷基芳基或芳基），所述烷基，环烷基，环烷基烷基，烷基芳基和芳基被官能团取代或不与R5取代; 或R 1和R 2一起形成环（该术语包括单环，二和更高多环系统）; R4是氢原子，烷基，芳基，烷基芳基，所述基团被卤素原子取代或不与Cl，Br或F取代; X是氧原子或离去基团，m是整数1或2; 当m为1时，X为离去基团; 当m为2时，X为氧原子，其包括：在非均相催化剂存在下的式（II）的肟衍生物，其中R 1，R 2和R 3如上所定义的肟衍生物与氢化/异构化反应，其中酰基衍生物为式（III）（R4CO）m X其中R4，m和X如上定义。

2. 发明申请

US20060052639A1 Process for the synthesis of indanylamine or aminotetralin derivatives and novel intermediates 失效
标题翻译：茚基胺或氨基四氢萘衍生物和新型中间体的合成方法
公开(公告)号：US20060052639A1
公开(公告)日：2006-03-09
申请号：US11221035
申请日：2005-09-07
申请人： Sylvie Blanchet , Bertrand Blandine , Alain Burgos , Yvon Derrien , Marie-Laure Moreau
发明人： Sylvie Blanchet , Bertrand Blandine , Alain Burgos , Yvon Derrien , Marie-Laure Moreau
IPC分类号： C07C231/02
CPC分类号： C07C213/02 , C07C231/08 , C07C231/10 , C07C233/23 , C07C251/64 , C07C251/66
摘要： A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.
摘要翻译：描述了通过用有机酸酰化肟，然后在有机酸存在下进行催化氢化随后水解从茚满酮或四氢萘酮肟制备茚满基胺和氨基四氢萘衍生物的方法。该方法在商业上可行，以高产率提供可用作生产治疗活性化合物的中间体的茚满胺和氨基四氢萘衍生物。还描述了新型中间体，1-二氢茚酮O-乙酰肟和1-四氢萘酮O-乙酰肟。

3. 发明授权

US07456320B2 Process for the synthesis of substituted alpha-aminoindan derivatives 有权
标题翻译：用于合成取代的α-氨基茚满衍生物的方法
公开(公告)号：US07456320B2
公开(公告)日：2008-11-25
申请号：US10589529
申请日：2005-02-21
申请人： Blandine Bertrand , Sylvie Blanchet , Alain Burgos , Juliette Martin , Florence Perrin , Sonia Roussiasse , Yvon Derrien
发明人： Blandine Bertrand , Sylvie Blanchet , Alain Burgos , Juliette Martin , Florence Perrin , Sonia Roussiasse , Yvon Derrien
IPC分类号： C07C209/62
CPC分类号： C07C213/02 , C07C217/54 , C07C233/25 , C07C2602/08
摘要： A process for the preparation of optically active substituted alpha-amino-indane derivatives of formula (I), which include: an asymmetric hydrogenation reaction of an en-amide derivative of formula (III) in presence of hydrogen and an optically active catalyst, in order to obtain an amide derivative of formula (II), a hydrolysis reaction of the amide derivative of formula (II) obtained in the previous step,in order to obtain optically active substituted alpha-amino-indane derivatives of formula (I).
摘要翻译：一种制备式（I）的光学活性取代的α-氨基 - 二氢化茚衍生物的方法，其包括：式（III）的酰胺衍生物在氢和光学活性催化剂存在下的不对称氢化反应，为了获得式（I）的光学活性取代的α-氨基 - 二氢茚衍生物，得到上述步骤中得到的式（II）的酰胺衍生物的水解反应，得到式（II）的酰胺衍生物。

4. 发明授权

US07262326B2 Process for the synthesis of indanylamine or aminotetralin derivatives and novel intermediates 失效
标题翻译：茚基胺或氨基四氢萘衍生物和新型中间体的合成方法
公开(公告)号：US07262326B2
公开(公告)日：2007-08-28
申请号：US11221035
申请日：2005-09-07
申请人： Sylvie Blanchet , Bertrand Blandine , Alain Burgos , Yvon Derrien , Marie-Laure Moreau
发明人： Sylvie Blanchet , Bertrand Blandine , Alain Burgos , Yvon Derrien , Marie-Laure Moreau
IPC分类号： C07C233/05
CPC分类号： C07C213/02 , C07C231/08 , C07C231/10 , C07C233/23 , C07C251/64 , C07C251/66
摘要： A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.
摘要翻译：描述了通过用有机酸酰化肟，然后在有机酸存在下进行催化氢化随后水解从茚满酮或四氢萘酮肟制备茚满基胺和氨基四氢萘衍生物的方法。该方法在商业上可行，以高产率提供可用作生产治疗活性化合物的中间体的茚满胺和氨基四氢萘衍生物。还描述了新型中间体，1-二氢茚酮O-乙酰肟和1-四氢萘酮O-乙酰肟。

5. 发明申请

US20070191640A1 Process for the synthesis of substituted alpha-aminoindan derivatives 有权
标题翻译：用于合成取代的α-氨基茚满衍生物的方法
公开(公告)号：US20070191640A1
公开(公告)日：2007-08-16
申请号：US10589529
申请日：2005-02-21
申请人： Blandine Bertrand , Sylvie Blanchet , Alain Burgos , Juliette Martin , Florence Perrin , Sonia Roussiasse , Yvon Derrien
发明人： Blandine Bertrand , Sylvie Blanchet , Alain Burgos , Juliette Martin , Florence Perrin , Sonia Roussiasse , Yvon Derrien
IPC分类号： C07C213/02
CPC分类号： C07C213/02 , C07C217/54 , C07C233/25 , C07C2602/08
摘要： A process is for the preparation of optically active substituted alpha-indanyl amide derivatives of formula (I), which include: an asymmetric hydrogenation reaction of an en-amide derivative of formula (III) in presence of hydrogen and an optically active catalyst, in order to obtain an amide derivative of formula (II), a hydrolysis reaction of the amide derivative of formula (II) obtained in the previous step, in order to obtain optically active-substituted alpha-indanyl amide derivatives of formula (I).
摘要翻译：一种制备式（I）的光学活性取代的α-茚满基酰胺衍生物的方法，其包括：式（III）的酰胺衍生物在氢和光学活性催化剂存在下的不对称氢化反应，为了获得式（I）的光学活性取代的α-茚满基酰胺衍生物，得到上述步骤中得到的式（II）的酰胺衍生物的水解反应，得到式（II）的酰胺衍生物。

6. 发明授权

US07884243B2 Process for the synthesis of eneamide derivatives 有权
标题翻译：合成烯酰胺衍生物的方法
公开(公告)号：US07884243B2
公开(公告)日：2011-02-08
申请号：US10583902
申请日：2004-12-22
申请人： Alain Burgos , Blandine Bertrand , Sonia Roussiasse , Jean-François Pluvie , Sylvie Blanchet , Juliette Martin , Florence Perrin , Françoise Bourdeau
发明人： Alain Burgos , Blandine Bertrand , Sonia Roussiasse , Jean-François Pluvie , Sylvie Blanchet , Juliette Martin , Florence Perrin , Françoise Bourdeau
IPC分类号： C07C233/00
CPC分类号： C07C231/10 , C07C233/06 , C07C2602/08 , C07C2602/10
摘要： A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isomerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) wherein R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)mX wherein R4, m and X are as defined above.
摘要翻译：制备由式（I）表示的烯 - 酰胺衍生物的方法，其中R 1和R 2和R 3独立地为氢原子，烷基，环烷基，环烷基烷基，烷基芳基，芳基，杂环，氰基，烷氧基，芳氧基，羧基，氨基甲酰基-CONR 5 R 6（其中R 5和R 6独立地是烷基，芳基烷基或芳基，所述环被取代或不被官能团或与R5）或-COOR5基团（其中 R5是烷基，烷基芳基或芳基），所述烷基，环烷基，环烷基烷基，烷基芳基和芳基被官能团取代或不与R5取代; 或R 1和R 2一起形成环（该术语包括单环，二和更高多环系）; R4是氢原子，烷基，芳基，烷基芳基，所述基团被卤素原子取代或未被取代为Cl，Br或F; X是氧原子或离去基团，m是整数1或2; 当m为1时，X为离去基团; 当m为2时，X为氧原子，其包括：在非均相催化剂存在下的氢化/异构化反应，式（II）的肟衍生物，其中R 1，R 2和R 3如上定义，与酰基衍生物式（III）（R4CO）mX其中R4，m和X如上所定义。

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