专利号:US-6800785-B1 优先权日:2002-10-15 标题:Process for the synthesis of estrogen receptor modulators 发明人:MENG DONGFANG 权利人:MERCK & CO INC 摘要:The present invention relates to processes for the synthesis of intermediates useful for the synthesis of estrogen receptor modulators. The process includes new methods for annelating 5-, 6- and 7-membered cycloalkenones onto an indanone.
专利号:US-8580975-B2 优先权日:2008-01-11 标 题:Synthesis of macrocyclic cancer chemotherapy agents and methods of use 发明人:GHOSH ARUN K; XU XIAOMING 权利人:GHOSH ARUN K; XU XIAOMING; PURDUE RESEARCH FOUNDATION 摘要:Herein are described a process for forming a quaternary carbon useful in the preparation of macrolactones, an enantioselective synthesis of (+)-peloruside A, and methods for treating a patient in need of relief from cancer or a cancer-related disease. The described processes are useful for preparing compounds containing quaternary carbons, including structural analogs and derivatives of peloruside A.
专利号:US-11708341-B2 优先权日:2016-08-05 标题:Synthesis of (S)-2-amino-4-methyl-((R)-2-methyloxirane-2-yl)-pentan-1-one and pharmaceutically acceptable salts thereof 发明人:Beaver Matthew; CUI SHENG; SHI XIANGQING 权利人:AMGEN INC 摘要:The present invention provides new methods for preparing compound 5, and pharmaceutically acceptable salts thereof, of structure n nCompound 5, or a pharmaceutically acceptable salt thereof, is an important intermediate in the synthesis of carfilzomib. The invention further provides methods of making a useful manganese catalyst that may be used in the epoxidation step of the present invention.
专利号:US-9968612-B2 优先权日:2012-09-17 标题:Method of synthesizing thyroid hormone analogs and polymorphs thereof 发明人:TAUB REBECCA; REYNOLDS CHARLES H 权利人:MADRIGAL PHARMACEUTICALS INC 摘要:The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.
专利号:US-2005256324-A1 优先权日:2004-05-10 标 题:Synthesis of amino acid keto-epoxides 发明人:LAIDIG GUY J; RADEL PEGGY A; SMYTH MARK S 权利人:PROTEOLIX INC 摘要:This invention relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.
专利号:WO-2018100050-A1 优先权日:2016-12-01 标 题 :Process for the preparation of an intermediate for the synthesis of carfilzomib 发明人:PASTÓ AGUILÀ Mireia; ÉCIJA QUERALT MARTA 权利人:ENANTIA S L 摘要:The present invention provides a compound which is the trichloroacetic acid salt of a compound of Formula (II) wherein R is selected from the group consisting of H, CH 3- , (CH 3 ) 2 CH-, (CH 3 ) 2 CHCH 2 -, CH 3 CH 2 CH(CH 3 )-, and PhCH 2 -, and a process for its preparation. Formula (II) Also provided is a process for its preparation based on the stereoselective epoxidation of the corresponding olefin precursor and a process for the preparation of several pharmaceutically active ingredients comprising the preparation of the compound of formula (II).
参考标题:Synthesis Of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, And 2-Pyrazolylbenzohydrazide Via 3-Substituted 3-Hydroxyisoindolin-1-Ones 作者:Hanh Nho Nguyen,Victor J. Cee,Holly L. Deak,Bingfan Du,Kathleen Panter Faber,Hakan Gunaydin,Brian L. Hodous,Steven L. Hollis,Paul H. Krolikowski,Philip R. Olivieri,Vinod F. Patel,Karina Romero,Laurie B. Schenkel,Stephanie D. Geuns-Meyer |发布日期:2012.4.20 摘要:Hydrazine, Followed By Chlorination With Pocl3. We Have Also Discovered Two Novel Transformations Of 3-Vinyl- And 3-Alkynyl-3-Hydroxyisoindolinones. Addition Of Vinyl Organometallic Reagents To N,N-Dimethylaminophthalimide (8A) Provided Dihydrobenzoazepinediones 15A-15C Via The Proposed Ring Expansion Of 3-Vinyl-3-Hydroxyisoindolinone Intermediates. 3-Alkynyl-3-Hydroxyisoindolinones React With Hydrazine And
合成参考文献
摘要:Negishi, E.; Wang, G., Science of Synthesis, (2009) 46, 266. 摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 47, 466. 摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 47, 468. 摘要:Gagnon, A.; Benoit, E.; Le Roch, A., Science of Synthesis Knowledge Updates, (2018) 4, 2. 摘要:Anderson, E. A.; Lim, D. S. W., Science of Synthesis Knowledge Updates, (2015) 1, 60.