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1. 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。

2. 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。

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。

5. 发明授权

US07365212B2 Method for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes which are used in asymmetric reduction reactions 失效
标题翻译：用于不对称还原反应的由恶唑硼烷 - 硼烷络合物衍生的手性化合物的原位制备方法
公开(公告)号：US07365212B2
公开(公告)日：2008-04-29
申请号：US10574871
申请日：2004-10-11
申请人： Alain Burgos , Blandine Bertrand , Stéphane Frein , Jean-François Pluvie , Sonia Roussiasse
发明人： Alain Burgos , Blandine Bertrand , Stéphane Frein , Jean-François Pluvie , Sonia Roussiasse
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , C07F5/022
摘要： A process for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes, wherein a metal borohydride, a Lewis base and an inorganic acid ester are brought together and an optically active amino alcohol and optionally a halide are then added. The compound obtained is a complex that is useful as a catalyst in asymmetric reduction reactions. The reaction is performed by adding the substance to be reduced, particularly prochiral ketones or ether oximes, in order to synthesize chiral alcohols or chiral amines.
摘要翻译：原位制备衍生自恶唑硼烷 - 硼烷络合物的手性化合物的方法，其中将金属硼氢化物，路易斯碱和无机酸酯引入到一起，然后加入光学活性氨基醇和任选的卤化物。获得的化合物是可用作不对称还原反应中的催化剂的络合物。通过加入待还原的物质，特别是前手性酮或醚肟进行反应，以合成手性醇或手性胺。

6. 发明申请

US20070055068A1 Method for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes which are used in asymmetric reduction reactions 失效
标题翻译：用于不对称还原反应的由恶唑硼烷 - 硼烷络合物衍生的手性化合物的原位制备方法
公开(公告)号：US20070055068A1
公开(公告)日：2007-03-08
申请号：US10574871
申请日：2004-10-11
申请人： Alain Burgos , Blandine Bertrand , Stephane Frein , Jean-Francois Pluvie , Sonia Roussiasse
发明人： Alain Burgos , Blandine Bertrand , Stephane Frein , Jean-Francois Pluvie , Sonia Roussiasse
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , C07F5/022
摘要： A process for the in situ preparation of chiral compounds derived from oxazaborolidine-borane complexes, wherein a metal borohydride, a Lewis base and an inorganic acid ester are brought together and an optically active amino alcohol and optionally a halide are then added. The compound obtained is a complex that is useful as a catalyst in asymmetric reduction reactions. The reaction is performed by adding the substance to be reduced, particularly prochiral ketones or ether oximes, in order to synthesize chiral alcohols or chiral amines.
摘要翻译：原位制备衍生自恶唑硼烷 - 硼烷络合物的手性化合物的方法，其中将金属硼氢化物，路易斯碱和无机酸酯引入到一起，然后加入光学活性氨基醇和任选的卤化物。获得的化合物是可用作不对称还原反应中的催化剂的络合物。通过加入待还原物质，特别是前手性酮或醚肟进行反应，以合成手性醇或手性胺。

7. 发明授权

US06861535B2 Cyclization method for the synthesis of pyrrolidine derivative compounds 有权
标题翻译：用于合成吡咯烷衍生物化合物的环化方法
公开(公告)号：US06861535B2
公开(公告)日：2005-03-01
申请号：US10449377
申请日：2003-05-30
申请人： Michel Bulliard , Blandine Laboue , Jean-Francois Pluvie , Sonia Roussiasse , Tony Pintus
发明人： Michel Bulliard , Blandine Laboue , Jean-Francois Pluvie , Sonia Roussiasse , Tony Pintus
IPC分类号： C07B61/00 , C07D207/08 , C07D207/12 , C07D207/00
CPC分类号： C07D207/12
摘要： A method for preparing pyrrolidine derivatives comprising cyclizing a compound of formula (I): in the presence of: a) a catalyst, b) a primary amine and c) a base, in a solvent to obtain pyrrolidine derivative of formula (II) below:
摘要翻译：一种制备吡咯烷衍生物的方法，其包括使式（I）化合物环化：在a）催化剂，b）伯胺和c）碱的存在下，在溶剂中得到下述式（II）的吡咯烷衍生物：

8. 发明授权

US06794525B2 Optically active chiral diphosphine ligands 失效
标题翻译：光学活性的手性二膦配体
公开(公告)号：US06794525B2
公开(公告)日：2004-09-21
申请号：US10356233
申请日：2003-01-31
申请人： Michel Bulliard , Blandine Laboue , Sonia Roussiasse
发明人： Michel Bulliard , Blandine Laboue , Sonia Roussiasse
IPC分类号： C07F1500
CPC分类号： C07F15/0053 , B01J31/2409 , B01J31/2414 , B01J2231/52 , B01J2231/643 , B01J2231/645 , B01J2531/0208 , B01J2531/0266 , B01J2531/26 , B01J2531/31 , B01J2531/42 , B01J2531/46 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07B53/00 , C07B2200/07 , C07C67/31 , C07F9/5027 , C07C69/732
摘要： An (R) or (S) chiral diphosphine of formula (I): wherein R and R1, which can be identical or different, represent an optionally saturated C1-10 alkyl group, an optionally saturated C3-9 cycloalkyl group, a C5-10 aryl group, the groups being optionally substituted by a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the alkyl, cycloalkyl, aryl groups optionally including one or more heteroatoms, or R and R1 together represent an optionally saturated C2-6 substituted alkyl group, an optionally saturated C3-9 cycloalkyl group, a C5-10 aryl group, the cycloalkyl or aryl groups being optionally substituted by a C1-5 alkyl, a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the alkyl, cycloalkyl, aryl groups optionally including one or more heteroatoms, R2 and R3, which can be identical or different, represent an optionally saturated C3-8 cycloalkyl group, a C6-10 aryl group, the groups being optionally substituted by a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the cycloalkyl, aryl groups optionally including one or more heteroatoms, or R2 and R3 together form an optionally saturated C4-8 cyclic group, a C6-10 aryl group, the groups being optionally substituted by a halogen, a hydroxy, a C1-5 alkoxy, an amino, a sulfino, a sulonfyl, with R4 representing an alkyl, an alkoxy or an alkylcarbonyl, the cyclic and aryl groups optionally including one or more heteroatoms.
摘要翻译：式（I）的（R）或（S）手性二膦：其中R和R 1可以相同或不同，表示任选饱和的C 1-10烷基，任选饱和的C 3-9环烷基， 10芳基，该基团任选被卤素，羟基，C 1-5烷氧基，氨基，亚磺酰基，磺酰基取代，R 4表示烷基，烷氧基或烷基羰基，烷基，环烷基，芳基任选地包括一个或多个杂原子，或R和R 1一起表示任选饱和的C 2-6取代烷基，任选饱和的C 3-9环烷基，C 5-10芳基，环烷基或芳基任选被C 1 -5-烷基，卤素，羟基，C 1-5烷氧基，氨基，亚磺酰基，磺酰基，其中R 4表示烷基，烷氧基或烷基羰基，烷基，环烷基，芳基，任选地包括一个或多个杂原子可以相同或不同的R 2和R 3表示任选饱和的 C 3〜C 8环烷基，C 6-10芳基，所述基团任选被卤素，羟基，C 1-5烷氧基，氨基，亚磺酰基，磺酰基取代，R 4表示烷基，烷氧基或烷基羰基，环烷基，任选地包括一个或多个杂原子的芳基，或者R 2和R 3一起形成任选饱和的C 4-8环基，C 6-10芳基，该基团任选被卤素取代，羟基， C 1-5烷氧基，氨基，亚磺酰基，磺酰基，其中R 4表示烷基，烷氧基或烷基羰基，环和芳基任选地包括一个或多个杂原子。

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