公开(公告)号：EP2885282A1

公开(公告)日：2015-06-24

申请号：EP13845790.8

申请日：2013-10-10

Applicant: Okinawa Institute of Science and Technology Graduate University

Inventor： CHOUTHAIWALE, Pandurang V. ,  TANAKA, Fujie

IPC: C07D309/30 ,  A61K31/215 ,  A61K31/351 ,  A61K31/357 ,  A61K31/498 ,  A61K31/551 ,  A61P35/00 ,  C07C201/14 ,  C07C205/55 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/28 ,  C07D317/30 ,  C07D407/04

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

Abstract: Disclosed is a process for preparing dihydro-2H-pyran derivatives of formula I: wherein R
1 and R
2 are defined herein. The process of the invention provides the compound of formula I in concise cascade reactions and in one pot. The compound of formulae I prepared by the process of the invention and its further transformed derivatives are useful for making pharmaceutical composition for the treatment of proliferative diseases.

公开(公告)号：EP1987880A1

公开(公告)日：2008-11-05

申请号：EP07714975.5

申请日：2007-02-27

Applicant: Japan Science and Technology Agency

Inventor： KOBAYASHI, Shu ,  OYAMADA, Hidekazu ,  AKIYAMA, Ryo ,  NAITO, Takeshi

IPC: B01J31/28 ,  B01J31/26 ,  B01J31/38 ,  B01J37/03 ,  B01J37/08 ,  B01J37/34 ,  C07C2/86 ,  C07C5/03 ,  C07C5/08 ,  C07C15/12 ,  C07C15/18 ,  C07C15/54 ,  C07C67/303 ,  C07C67/343 ,  C07C69/612 ,  C07C69/618 ,  C07C201/14 ,  C07C205/19 ,  C07F7/08 ,  C07F7/18 ,  C07B61/00

CPC classification number: C07C67/303 ,  B01J23/40 ,  B01J23/70 ,  B01J31/124 ,  B01J31/127 ,  B01J31/165 ,  B01J31/26 ,  B01J31/28 ,  B01J35/006 ,  B01J37/0219 ,  B01J2231/4261 ,  B01J2231/641 ,  B01J2531/824 ,  B01J2531/828 ,  C07B2200/11 ,  C07C2/861 ,  C07C5/03 ,  C07C5/08 ,  C07C67/343 ,  C07C205/19 ,  C07C2523/42 ,  C07C2523/44 ,  C07C2523/72 ,  C07F15/0066 ,  C07F15/0086 ,  C07F15/0093 ,  C07C15/54 ,  C07C15/18 ,  C07C69/612 ,  C07C69/618

Abstract: The present invention provides a polysilane-supported transition metal catalysts or a polysilane/inorganic compound-supported transition metal catalysts, wherein various types of transition metals are supported by polysilane compounds, or combination of polysilanes and inorganic compounds. The catalysts of the present invention are hardly soluble in hydrocarbons and alcohols and are useful as catalysts in heterogeneous system for various organic synthetic reactions using the above solvents. Polysilanes supporting transition metals are easily crosslinkable by thermal treatment, microwave irradiation, UV irradiation or chemical methods such as hydrosilylation reaction and are changed to be insoluble in various solvents keeping high catalytic activity. Moreover, the stability and operability of polysilane-supported transition metal catalysts will be improved by the support thereof on inorganic compounds. These polysilane-supported transition metal catalysts show a high catalytic activity in hydrogenation reaction, hydrosilylation reaction, Heck reaction, Suzuki-Miyaura coupling reactions and the like. The catalyst is easily recoverable and reusable and the leakage of metals is extremely few.

Abstract translation: 本发明提供一种聚硅烷负载的过渡金属催化剂或聚硅烷/无机化合物负载的过渡金属催化剂，其中各种类型的过渡金属由聚硅烷化合物或聚硅烷和无机化合物的组合负载。 本发明的催化剂几乎不溶于烃和醇，并且可用作用于使用上述溶剂的各种有机合成反应的异相体系中的催化剂。 支撑过渡金属的聚硅烷通过热处理，微波照射，UV照射或氢化硅烷化反应等化学方法易于交联，并且改变为不溶于保持高催化活性的各种溶剂中。 此外，通过其对无机化合物的支持，聚硅烷负载的过渡金属催化剂的稳定性和可操作性将得到改善。 这些聚硅烷负载的过渡金属催化剂在氢化反应，氢化硅烷化反应，Heck反应，Suzuki-Miyaura偶联反应等中显示出高的催化活性。 催化剂易于回收和再利用，金属的泄漏极少。

公开(公告)号：EP2885282B1

公开(公告)日：2017-03-15

申请号：EP13845790.8

申请日：2013-10-10

Applicant: Okinawa Institute of Science and Technology School Corporation

Inventor： CHOUTHAIWALE, Pandurang V. ,  TANAKA, Fujie

IPC: C07D309/30 ,  A61K31/215 ,  A61K31/351 ,  A61K31/357 ,  A61K31/498 ,  A61K31/551 ,  A61P35/00 ,  C07C201/14 ,  C07C205/55 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/28 ,  C07D317/30 ,  C07D407/04

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

公开(公告)号：EP2885282A4

公开(公告)日：2016-01-27

申请号：EP13845790

申请日：2013-10-10

Applicant: OKINAWA INST OF SCIENCE AND TECHNOLOGY GRADUATE UNIVERSITY

Inventor： CHOUTHAIWALE PANDURANG V ,  TANAKA FUJIE

IPC: C07D309/30 ,  A61K31/215 ,  A61K31/351 ,  A61K31/357 ,  A61K31/498 ,  A61K31/551 ,  A61P35/00 ,  C07C201/14 ,  C07C205/55 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/28 ,  C07D317/30 ,  C07D407/04

CPC classification number: C07D309/28 ,  C07C201/14 ,  C07C205/55 ,  C07C2601/14 ,  C07D241/44 ,  C07D243/02 ,  C07D307/54 ,  C07D309/30 ,  C07D317/30 ,  C07D407/04

公开(公告)号：EP2491000B1

公开(公告)日：2015-11-25

申请号：EP10765718.1

申请日：2010-10-06

Applicant: ANGUS Chemical Company

Inventor： TRAUTH, Daniel, M. ,  GREEN, George, D. ,  SWEDO, Raymond, J.

IPC: C07C205/02 ,  C07C201/08 ,  C07C201/14

CPC classification number: C07C201/08 ,  Y02P20/582 ,  C07C205/02

公开(公告)号：EP1700859A2

公开(公告)日：2006-09-13

申请号：EP06013051.5

申请日：2001-07-26

Applicant: Shire US Inc.

Inventor： Lang, Philip Charles ,  Spencer, Roxanne Paula ,  Yeh, Wen-Lung ,  Roth, Michael Joseph

IPC: C07D487/04 ,  C07C209/36 ,  C07C201/08 ,  C07C201/12 ,  C07C201/14

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making certain 6,7-dihalo-1,5-dihydroimidazo [2,1-b]quinazolin-2 (3H)-ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6-nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnCl 2 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones from the corresponding iminoquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.

Abstract translation: 提供了从2,3-二卤代苯甲醛制备某些6,7-二卤代-1,5-二氢咪唑并[2,1-b]喹唑啉-2（3H） - 酮的方法。 还提供了一种从2,3-二卤代苯甲醛制备中间体N-（2,3-二卤代-6-硝基苄基）甘氨酸的甘氨酸，并使用SnCl 2或特别限定的催化剂还原甘氨酸化合物的方法。 进一步提供从相应的亚氨基喹唑啉化合物形成所需的6,7-二卤代-1,5-二氢咪唑并[2,1-b]喹唑啉-2（3H） - 酮的环化方法。 这些方法特别适用于制造阿那格雷碱。

公开(公告)号：EP0402485A4

公开(公告)日：1991-01-23

申请号：EP90901095

申请日：1989-12-22

Applicant: ANDRIEVSKY, ALEXANDR MIKHAILOVICH ,  GORELIK, MIKHAIL VIKTOROVICH ,  AVIDON, SERGEI VIKTOROVICH ,  GORDIEVSKAYA, EVGENIA VASILIEVNA ,  ALTMAN, ELENA SHULIMOVNA ,  VOROZHTSOV, GEORGY NIKOLAEVICH ,  DJUMAEV, KIRILL MIKHAILOVICH

Inventor： ANDRIEVSKY, ALEXANDR MIKHAILOVICH ,  GORELIK, MIKHAIL VIKTOROVICH ,  AVIDON, SERGEI VIKTOROVICH ,  GORDIEVSKAYA, EVGENIA VASILIEVNA ,  ALTMAN, ELENA SHULIMOVNA ,  VOROZHTSOV, GEORGY NIKOLAEVICH ,  DJUMAEV, KIRILL MIKHAILOVICH

IPC: C07C201/14 ,  C07C205/12 ,  C07B39/00 ,  C07B43/02 ,  C07C201/06 ,  C07C201/08

CPC classification number: C07C201/14 ,  C07C205/12

公开(公告)号：EP4387951A1

公开(公告)日：2024-06-26

申请号：EP22768536.9

申请日：2022-08-17

Applicant: Amgen Inc.

Inventor： ORTIZ, Adrian ,  DOERFLER, Jaika ,  VAIDA, Karina R.

IPC: C07C201/14 ,  C07C205/58 ,  C07C319/14 ,  C07C319/20 ,  C07C323/62 ,  C07C323/63 ,  C12P13/00

CPC classification number: C07C201/14 ,  C07C319/14 ,  C07C323/63 ,  C07C319/20 ,  C12P13/001

公开(公告)号：EP1700859A3

公开(公告)日：2010-02-24

申请号：EP06013051.5

申请日：2001-07-26

Applicant: Shire US Inc.

Inventor： Lang, Philip Charles ,  Spencer, Roxanne Paula ,  Yeh, Wen-Lung ,  Roth, Michael Joseph

IPC: C07D487/04 ,  C07C209/36 ,  C07C201/08 ,  C07C201/12 ,  C07C201/14

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making certain 6,7-dihalo-1,5-dihydroimidazo [2,1-b]quinazolin-2 (3H)-ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6-nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnCl 2 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones from the corresponding iminoquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.

Abstract translation: 提供了从2,3-二卤代苯甲醛制备某些6,7-二卤代-1,5-二氢咪唑并[2,1-b]喹唑啉-2（3H） - 酮的方法。 还提供了从2,3-二卤代苯甲醛制备中间体N-（2,3-二卤代-6-硝基苄基）甘氨酸和使用SnCl2或特定催化剂还原甘氨酸化合物的方法。 进一步提供从相应的亚氨基喹唑啉化合物形成所需的6,7-二卤代-1,5-二氢咪唑并[2,1-b]喹唑啉-2（3H） - 酮的环化方法。 这些方法特别适用于制造阿那格雷碱。

公开(公告)号：EP1700843A3

公开(公告)日：2010-02-24

申请号：EP06013053.1

申请日：2001-07-26

Applicant: Shire US Inc.

Inventor： Lang, Philip Charles ,  Spencer, Roxanne Paula ,  Yeh, Wen-Lung ,  Roth, Michael Jopseph

IPC: C07C209/36 ,  C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C201/14

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making certain 6,7-dihalo-1,5-dihydroimidazo [2,1-b] quinazolin-2(3H)-ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6-nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnCl 2 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones from the corresponding iminoquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.