专利号:US-9187408-B2 优先权日:2008-10-27 标 题 :Process for the preparation of protected L-alanine derivatives 发明人:ANZALONE LUIGI; FEIBUSH PENINA; VILLANI FRANK J 权利人:JANSSEN PHARMACEUTICA NV; JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.
专利号:US-8633182-B2 优先权日:2012-05-30 标题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN 权利人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-9051289-B2 优先权日:2013-09-26 标 题 :Process and intermediates for preparing GPR40 agonists 发明人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN 权利人:DAHMANN GEORG; WAGNER HOLGER; ECKHARDT MATTHIAS; FRANK MARKUS; SANTAGOSTINO MARCO; SCHNAUBELT JUERGEN; STERTZ UWE; PACHUR THORSTEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of formula I n nwherein R S denotes F or CF 3 , R a denotes H or C 1-4 -alkyl and Z denotes a leaving group or an optionally substituted or protected hydroxyl group, suitable as intermediates in the synthesis of indanyloxydihydrobenzofuranylacetic acids, which are GPR40 agonists, to a process for preparing these intermediates and to the process for preparing the GPR40 agonists making use of an asymmetric catalytic hydrogenation reaction in the presence of a transition metal catalyst and a chiral auxiliary.
专利号:US-9308194-B2 优先权日:2013-11-28 标 题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:LINGARD IAIN; HAMPRECHT DIETER 权利人:BOEHRINGER INGELHEIM INT 摘要:A compound of formula I, n nwherein the groups R 1 , R 2 , R 3 , X, m, and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
参考标题:An Efficient Method For Sterically Demanding Suzuki-Miyaura Coupling Reactions 作者:Qing Zhao,Chengxi Li,Chris H. Senanayake,Wenjun Tang |发布日期:2013.2.11 摘要:An Efficient Method For Sterically Demanding Suzuki-Miyaura Coupling Reactions Has Been Developed With Two Catalysts, Pd/bi‐dime (See Scheme) And Pd/phenanthrene‐based Ligand. The Pd/bi‐dime Catalyst Facilitates The Syntheses Of Extremely Hindered Biaryls Bearing Ortho‐isopropyl Substituents. The Other Catalyst Is Efficient For The Synthesis Of Functionalized Tetra‐ortho‐substituted Biaryls At Low
合成参考文献
参考文献:10.1107/s2056989016017485 摘要:Navarrete Guitérrez A, Aguirre Hernández G, Bernès S. Crystal structures of p-substituted derivatives of 2,6-di-methyl-bromo-benzene with ½ ≤ Z' ≤ 4. Acta Crystallogr E Crystallogr Commun. 2016 Dec 01;72(Pt 12):1762–7.