4-氯乙酰乙酸甲酯置于盐酸,Sodium Methylate体系中,用 水,乙腈 作为反应溶剂,以91.7%的收率获得产物4-甲氧基乙酰乙酸甲酯 参考文献:Process For The Production Of 4-Alkoxyacetoacetic Acid Esters 标题:Process For The Production Of 4-Alkoxyacetoacetic Acid Esters 摘要:从4-氯或4-溴乙酰乙酸酯制备4-烷氧基乙酰乙酸酯的过程.将4-氯或4-溴乙酰乙酸酯与多于一个当量的碱性醇酸盐在无极溶剂中反应,有效温度为50oc至100oc.
专利号:US-2007015260-A1 优先权日:2002-03-14 标 题:Synthesis of synthons for the manufacture of bioactive compounds 发明人:WONG CHI-HUEY; LIU JUNJIE; DESANTIS GRACE; BURK MARK 权利人:SCRIPPS RESEARCH INST 摘要:The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.
专利号:US-4841042-A 优先权日:1985-03-19 标 题 :Process for the preparation of carbapenem intermediates 发明人:HAEBICH DIETER; HARTWIG WOLFGANG 权利人:BAYER AG 摘要:A process for the preparation of a 4-[3-carboxy-3-diazo-2-oxopropyl]azetidin-2-one of the formula ##STR1## comprising reacting a 4-acetoxy-2-azetininone of the formula ##STR2## with a compound of the formula ##STR3## in an inert solvent, in the presence of a base and of a silylating agent, in a one-pot process. n Many of the products are new. The products are useful in the synthesis of carbapenem antibiotics.
专利号:WO-2015019310-A1 优先权日:2013-08-07 标 题 :Process for the preparation of dolute-gravir and intermediates thereof 发明人:DANDALA RAMESH; VELLANKI SIVA RAM PRASAD; NADELLA MADHU MURTHY; BALUSU PHANI KUMAR 权利人:MYLAN LAB LTD 摘要:The present disclosure relates to processes for the preparation of dolutegravir or of its pharmaceutically acceptable salts. The present disclosure also provides intermediates useful in the synthesis of dolutegravir.
专利号:US-6642390-B2 优先权日:2001-07-11 标 题:One step synthesis of 1,2,3-triazole carboxylic acids 发明人:KOLB HARTMUTH C; CAVALLARO CULLEN; SHI ZHI-CAI; GONTCHAROV ALEXANDER; WANG ZHI-MIN; RICHARDSON PAUL F; KANAMARLAPUDI RAMANAIAH C 权利人:LEXICON PHARMACEUTICALS INC 摘要:Disclosed is a one step method for preparing a 1,2,3-triazole carboxylic acid by treating an azide with a beta-ketoester in the presence of a base.
专利号:US-2003232416-A1 优先权日:2002-03-14 标题:Synthesis of synthons for the manufacture of bioactive compounds
专利号:US-2003135050-A1 优先权日:2001-07-11 标题 :One step synthesis of 1,2,3-triazole carboxylic acids
参考标题:Rh(III)-Catalyzed Regio- And Chemoselective [4 + 1]-Annulation Of Azoxy Compounds With Diazoesters For The Synthesis Of 2H-Indazoles: Roles Of The Azoxy Oxygen Atom 作者:Zhen Long,Zhigang Wang,Danni Zhou,Danyang Wan,Jingsong You |发布日期:2017.6.2 摘要:Tandem C-H Alkylation/intramolecular Decarboxylative Cyclization Of Azoxy Compounds With Diazoesters For The Synthesis Of 3-Acyl-2H-Indazoles Is Disclosed. The Azoxy Instead Of The Azo Group Enables A Distinct Approach For Cyclative Capture, Leading To A [4 + 1]-Annulation Rather Than A Classic [4 + 2] Manner. The Azoxy Oxygen Atom Is Traceless After Annulation, And Further Removal From The Product Is
合成参考文献
摘要:Arai, N.; Ohkuma, T., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 16. 摘要:Wu, X.; Xiao, J., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 264.