专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:WO-2017033128-A1 优先权日:2015-08-25 标题 :Biphenyl-substitued 4-amino-butyric acid derivatives and their use in the synthesis of nep inhibitors 发明人:HOOK DAVID; KU JIE; ZHOU JIANGUANG 权利人:NOVARTIS AG; HOOK DAVID; KU JIE; ZHOU JIANGUANG 摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors and prodrugs thereof.
专利号:EP-1730108-B1 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin d analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
专利号:EP-1735276-B1 优先权日:2004-04-02 标题:Novel method for the preparation of intermediates useful for the synthesis of vitamin d analogues 发明人:HANSEN ERIK TORNGAARD; SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; PEDERSEN HENRIK; DEUSSEN HEINZ-JOSEF WILHELM 权利人:LEO PHARMA AS 摘要:The present invention relates to novel methods for the preparation of intermediates which are useful in the synthesis of cacipotriol. The present invention relates further to the use of intermediates produced with said methods for making calcipotriol or calcipotriol monohydrate.
专利号:US-8759555-B2 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin D analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
专利号:US-6117993-A 优先权日:1995-05-23 标题 :Synthons for oligonucleotide synthesis 发明人:IYER RADHAKRISHNAN P; YU DONG; GUO MAO-JUN; AGRAWAL SUDHIR 权利人:HYBRIDON INC 摘要:The invention provides new reagents and processes for synthesizing oligonucleotides, including stereoselective oligonucleotide synthesis. In a first aspect, the invention provides novel monomer synthons for the synthesis of oligonucleotides. Monomer synthons according to this aspect of the invention are useful in the synthesis of oligonucleotides and can be used in place of the well known beta-cyanoethyl phosphoramidite monomer synthon in the phosphoramidite synthesis procedure. Certain monomer synthons according to this aspect of the invention are useful in this procedure for producing oligonucleotides having defined stereochemistry. n In a second aspect, the invention provides processes for synthesizing monomer synthons according to the invention, including diastereomerically enriched or purified monomer synthons. In the processes according to this aspect of the invention, the chemical reactions are stereoretentive so that the products of each reaction retain the same stereoconfiguration as their precursor reagent. n In a third aspect, the invention provides processes for synthesizing oligonucleotides using the well known phosphoramidite approach. In the processes according to this aspect of the invention, any of the monomer synthons according to the invention is used in place of the conventional beta-cyanoethyl phosphoramidite.
参考标题:The Enantioselective Birch−cope Sequence For The Synthesis Of Carbocyclic Quaternary Stereocenters. Application To The Synthesis Of (+)-Mesembrine 作者:Tapas Paul,William P. Malachowski,Jisun Lee |发布日期:2006.8.1 摘要:A Synthetic Technique For Generating Carbocyclic Quaternary Stereocenters With Exceptionally High Levels Of Enantioselectivity Is Described. A Sequence Of Three Reactions, Enantioselective Birch Reduction-Allylation, Enol Ether Hydrolysis, And Cope Rearrangement, Is Used To Stereoselectively Generate Chiral Quaternary Centers On A 2-Cyclohexen-1-One Ring. The Products Of The Sequence Are 4,4-Disub