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CAS号335-05-7 三氟甲烷磺酰氟 | CAS号74-89-5 氨基甲烷 | CAS号358-23-6 三氟甲磺酸酐 | CAS号421-83-0 三氟甲烷磺酰氯合成工艺路线路线简述
- 合成目标产物 N-Methyltrifluoromethanesulfonamide 主要起始原料 Trifluoromethanesulfonic Anhydride And Methylamine Hydrochloride
- (文献来源)合成步骤主要原料 Trifluoromethanesulfonic Anhydride 和 Methylamine Hydrochloride
三氟甲磺酸酐,盐酸甲胺置于三乙胺体系中,用 二氯甲烷 作为反应溶剂,以11%的收率获得产物n-甲基三氟甲烷磺酰胺
参考文献:光氧化还原催化的伯胺衍生物的位点选择性α-C(sp3)-H烷基化.
标题:光氧化还原催化的伯胺衍生物的位点选择性α-C(sp3)-H烷基化.
摘要:叔胺在氧化反应中产生α-氨基自由基的合成作用已得到很好的确立,但是由于竞争性副反应,伯胺仍然具有挑战性.本报告介绍了通过反应生成α-氨基自由基中间体对伯胺衍生物进行的位点选择性α-官能化.通过可见光光氧化还原催化,伯磺酰胺与缺电子的烯烃结合,可以有效,温和地构建c-C键.有趣的是,通过保护基团的精确操作,观测到分子间氢原子转移(hat)催化与分子内[1,5] Hat之间的差异.利用这种二分法可实现出色的α/δ位点选择性.
DOI:10.1002/anie.201812227
专利信息
专利号:US-10266503-B1
优先权日:2016-05-24
标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins
发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN
权利人:UNIV ILLINOIS
摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.
专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人:MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-5721255-A
优先权日:1992-08-19
标 题 :Substituted benzylamino nitrogen containing non-aromatic heterocycles
发明人:HOWARD HARRY R; NAKANE MASAMI; IKUNAKA MASAYA; SATAKE KUNIO; ROSEN TERRY J; LOWE III JOHN A; O'NEILL BRIAN T; ITO FUMITAKA
权利人:PFIZER
摘要:The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R 1 , R 2 , R 3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
专利号:EP-0582908-B1
优先权日:1992-08-11
标 题 :2-Substituted quinolylmethoxy-phenylacetic acid- and -benzylacyl derivatives, process for their preparation and their use as inhibitors of leukotriene synthesis