4-溴-3,5-二氯苯胺 反应生成1-溴-2,6-二氯苯 参考文献:Hurtley,Journal Of The Chemical Society,1901,Vol. 79,P. 1303 标题:Hurtley,Journal Of The Chemical Society,1901,Vol. 79,P. 1303
专利号:US-2006111438-A1 优先权日:2004-10-21 标 题:Asymmetric synthesis of substituted dihydrobenzofurans 发明人:GONTCHAROV ALEXANDER V; KHAFIZOVA GULNAZ; POTOSKI JOHN R; YU QING; SHAW CHIA-CHENG; STACK GARY P; ZHOU DAHUI 权利人:WYETH CORP 摘要:The present invention concerns production of a compound of the formula n n nor a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula: n n nwhere Ar, Y, R 1 , R y , R 2 , and m are as defined herein.
专利号:US-6828466-B2 优先权日:2002-07-19 标题:Process for the synthesis of phenols from arenes 发明人:MALECZKA JR ROBERT E; SMITH III MILTON R; HOLMES DANIEL; SHI FENG 权利人:UNIV MICHIGAN STATE 摘要:A process to synthesize substituted phenols such as those of the general formula RR'R''Ar(OH) wherein R, R', and R'' are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C-H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
专利号:JP-H06316550-A 优先权日:1992-11-25 标题:Synthesis of deactivated anilines
专利号:AU-2005299884-A1 优先权日:2004-10-21 标 题 :Asymmetric synthesis of substituted dihydrobenzofurans
专利号:JP-2008517919-A 优先权日:2004-10-21 标题 :Asymmetric synthesis of substituted dihydrobenzofurans.