专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:WO-2010146391-A1 优先权日:2009-06-15 标题:Regioselective synthesis of letrozole 发明人:GORE VINAYAK GOVIND; SHUKLA VINAY KUMAR; BHANDARI SHERYAS; HASBE SURESH; MEKDE SANDEEP 权利人:GENERICS UK LTD; MYLAN INDIA PRIVATE LTD; GORE VINAYAK GOVIND; SHUKLA VINAY KUMAR; BHANDARI SHERYAS; HASBE SURESH; MEKDE SANDEEP 摘要:The present invention relates to an improved process for the preparation of letrozole (I) and its pharmaceutically acceptable salts, to compositions comprising letrozole or a pharmaceutically acceptable salt thereof, and to uses of such compositions. In particular it relates to a process and to novel intermediates for preparing letrozole and its salts substantially free from regioisomeric impurities.
专利号:US-8193392-B2 优先权日:2005-07-29 标 题:Method for enantioselective synthesis of phosphorus-stereogenic phosphines 发明人:SCRIBAN CORINA; GLUECK DAVID S 权利人:SCRIBAN CORINA; GLUECK DAVID S; DARTMOUTH COLLEGE 摘要:The present invention relates to a process for preparing an enantioenriched phosphorus-stereogenic, tertiary phosphine. Secondary phosphines are contacted with an alkyl halide and base in the presence of a chiral metal catalyst thereby producing the enantioenriched phosphorus-stereogenic, tertiary phosphine for subsequent use in homogeneous catalysis reactions.
专利号:WO-2015092739-A1 优先权日:2013-12-19 标题:Process for preparation of alogliptin 发明人:VADALI LAKSHMANA RAO; DASARI SRINIVASA RAO; MANUKONDA SESHADRI RAO; PONDURI RAJASEKHAR 权利人:MYLAN LAB LTD 摘要:Processes for the preparation of alogliptin benzoate are disclosed. The present disclosure also provides intermediates useful in the synthesis of alogliptin benzoate.
专利号:US-2014303333-A1 优先权日:2011-10-14 标题:Iron bisphenolate complexes and methods of use and synthesis thereof 发明人:SHAVER MICHAEL P; KOZAK CHRISTOPHER M 权利人:UNIV PRINCE EDWARD ISLAND; GENESIS GROUP INC 摘要:The present application, relates to iron bisphenolate complexes and methods of use and synthesis thereof. The iron complexes are prepared from tridentate or tetradentate ligands of Formula I: wherein R 1 and R 2 are as defined herein. Also provided are methods and processes of using the iron bisphenolate complexes as catalysts in cross-coupling reactions and in controlled radical polymerizations.
专利号:US-5939392-A 优先权日:1993-06-03 标 题 :Method of thrombin inhibition 发明人:ANTONSSON KARL THOMAS; BYLUND RUTH ELVY; GUSTAFSSON NILS DAVID; NILSSON NILS OLOV INGEMAR 权利人:ASTRA AB 摘要:The invention relates to new competitive tripeptide inhibitors of trypsin-like serine proteases, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory inhibitors for prophylaxis and treatment of related diseases.
[参考文献]: Prakash G Jagtap, Et Al. Facile And Convenient Syntheses Of 6,11-Dihydro-5H-Indeno[参考文献]: William L Scott, Et Al. Distributed Drug Discovery, Part 2: Global Rehearsal Of Alkylating Agents For The Synthesis Of Resin-Bound Unnatural Amino Acids And Virtual D(3) Catalog Construction. J Comb Chem. 2009 Jan-Feb;11(1):14-33.
合成参考文献
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