苯甲酸乙酯置于chromium(Vi) Oxide,硫酸,碘体系中,用 乙酸酐,溶剂黄146 作为反应溶剂,化学反应 4.0H,以64%的收率获得产物3-碘苯甲酸乙酯 参考文献:The Direct Iodination Of Arenes With Chromium(Vi) Oxide As The Oxidant 标题:The Direct Iodination Of Arenes With Chromium(Vi) Oxide As The Oxidant 摘要:提出了一种简单且便宜的实验室方法,用于许多活性和非活性芳香烃的直接单碘化和双碘化.主要的碘化反应在不超过65oc的温度下进行,反应时间为0.5至12小时,在无水的强酸性液体体系i2/acoh/ac2O/h2So4中进行,同时加入预先溶解的cro3作为氧化剂.纯碘化产物的产率从31%(对于3,5-二碘苯甲酸)到90%(对于4-碘乙醚)不等.至今,苯腈和一些可氧化的芳香族化合物,如萘,萘烷,黄烷和噻吩,被发现不适合有效碘化.然而,这种新颖,简单的直接碘化方法值得推广到其他适合的芳香族化合物. DOI:10.1246/bcsj.70.1665
专利号:US-2009082582-A1 优先权日:2006-03-14 标 题 :Process For Preparing [2-(2,3- Dihydrobenzofuran - Or Benzofuran-7-Yloxy)Ethyl]-(3 -Cyclopent-1-Ylbenzyl)Amine Derivatives and Synthesis Intermediate 发明人:VACHER BERNARD; CUISIAT STEPHANE; ROQUES NICOLAS 权利人:PF MEDICAMENT 摘要:The invention relates to a process for the preparation of compounds of general formula (3) n n n n n n n n n n wherein:n (a) represents a single or double bond; W represents a group CH, CH 2 , CHCH 3 , CCH 3 , C(CH 3 ) 2 , a group C(CH 2 ) 2 (i.e. a carbon atom carrying two methylene groups bonded to one another so as to form a spiro-cyclopropane moiety), with the proviso, however, that when (a) is a double bond then W represents exclusively a group CH or CCH 3 and when (a) is a single bond then W represents exclusively a group CH 2 , CHCH 3 , C(CH 3 ) 2 or C(CH 2 ) 2 .
专利号:JP-2005047864-A 优先权日:2003-07-30 标 题:New synthesis of aromatic olefins
专利号:US-2010010219-A1 优先权日:2006-12-07 标 题 :Method for producing pyrrolidine compound 发明人:HARADA KAZUHITO; ITO TAKASHI 权利人:JAPAN TOBACCO INC 摘要:Provided is a method capable of efficiently producing a compound having a superior HSD1 inhibitory action and a compound useful as a synthetic intermediate therefor, with superior achievability of asymmetric synthesis (i.e., superior selectivity), superior yield, superior safety and superior industrial workability at a low cost. n A method of producing a compound represented by the following formula [8]: n n n n n n n n n n or a salt thereof, or a solvate thereof, from a compound represented by the following formula [2]: n n n n n n n n n n or a reactive derivative thereof, or a salt thereof, or a solvate thereof.
[参考文献]: Shinya Fujii, Et Al. Acidic Heterocycles As Novel Hydrophilic Pharmacophore Of Androgen Receptor Ligands With A Carborane Core Structure. Bioorg Med Chem. 2009 Jan 1;17(1):344-50.
合成参考文献
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