专利号:US-5510528-A 优先权日:1993-04-08 标题:Preparation of halomethylbenzoly cyanides and novel halomethylbenzoyl cyanides 发明人:ISAK HEINZ; WETTLING THOMAS; KEIL MICHAEL; WOLF BERND; DOETZER REINHARD 权利人:BASF AG 摘要:A process for preparing halomethylbenzoyl cyanides I n n Ph-CO-CN I n n (Ph=phenyl radical substituted by chloromethyl or bromomethyl which, if desired, can additionally carry 1-4 further radicals) by reacting halomethylbenzoyl chlorides II n n Ph-CO-Cl II n n with an alkali metal cyanide or transition metal cyanide, if appropriate in an organic diluent, and novel halomethylbenzoyl cyanides I' ##STR1## (X=halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, CF 3 , C 1 -C 5 -alkyl-(C 1 -C 5 -alkyl)hydroxyimino or C 1 -C 5 -alkyl-(C 2 -C 5 -alkenyl)hydroxyimino; m=0 to 4 and Y=chloromethyl or bromomethyl) are described. n The halomethylbenzoyl cyanides I are important intermediates for the synthesis of plant protection agents.
专利号:US-7098342-B2 优先权日:2003-10-16 标题 :Preparation of candesartan cilexetil 发明人:ETINGER MARINA YU; FEDOTEV BORIS; DOLITZKY BEN-ZION 权利人:TEVA PHARMA 摘要:The invention encompasses processes for the synthesis of cilexetil trityl candesartan from the reaction of trityl candesartan with cilexetil halide in the presence of a base and a low boiling organic solvent. Optionally, the reaction may be conducted in the presence of a phase transfer catalyst.
专利号:US-2008241949-A1 优先权日:2007-03-29 标 题 :Process for preparing quetiapine fumarate 发明人:KANSAL VINOD KUMAR; AHMAD SUHAIL; LAL KANHAIYA; PATIL BHATU TUMBA 权利人:KANSAL VINOD KUMAR; AHMAD SUHAIL; LAL KANHAIYA; PATIL BHATU TUMBA 摘要:Provided is an improved synthesis of quetiapine and pharmaceutically acceptable salts.
专利号:US-7687622-B2 优先权日:2005-04-14 标 题 :Process for preparing quetiapine fumarate 发明人:KANSAL VINOD KUMAR; LAL KANHAIYA; AHMAD SUHAIL; LEONOV DAVID 权利人:TEVA PHARMA 摘要:Provided is a novel synthesis of quetiapine, and pharmaceutically acceptable salts thereof, in which an alkali metal halide or siliyl halide is included in the reaction mixture.
参考标题:Bioactive Indanes: Proof Of Concept Study For Enantioselective Synthetic Routes To Ph46A, A New Potential Anti-Inflammatory Agent 作者:Tao Zhang,Gaia Scalabrino,Neil Frankish,Helen Sheridan 摘要:Proof Of Principle For A Chiral Alkylation Of Ketone 3 Using Phase-Transfer Catalysis, Providing A Key Intermediate Ketone (S)-4. The Parent Alkaloids Required For The Synthesis Of Ph46A, Quinine Or Cinchonidine, Have Also Been Identified. Promising Enantiomeric Excesses Of Up To 50% Have Been Achieved To Date, And The Use Of An Alternative Substrate, Unsaturated Ketone 9, Has Also Opened Up Further Avenues
合成参考文献
摘要:Ogura, K., Science of Synthesis, (2007) 30, 453.