三氟甲苯置于氯,三氯化铁体系中,化学反应生成 间氯三氟甲苯 参考文献:Mcbee Et Al.,Journal Of The American Chemical Society,1947,Vol. 69,P. 946 标题:Mcbee Et Al.,Journal Of The American Chemical Society,1947,Vol. 69,P. 946
专利号:US-6958420-B2 优先权日:2002-07-19 标题:Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof 发明人:MALECZKA JR ROBERT E; SMITH III MILTON R; HOLMES DANIEL 权利人:UNIV MICHIGAN STATE 摘要:A process is described for synthesizing aminoarylboronic esters of the general formula n n nwherein R, R 2 , and R 3 are each an alkyl, aryl, vinyl, alkoxy, carboxylic esters, amides, or halogen; Ar is any variety of phenyl, naphthyl, anthracyl, heteroaryl; and R 1 is alkyl, hydrogen, or aryl. The aminoarylboronic esters are produced via the metal-catalyzed coupling of arylboronic esters of the general formula n n nwherein R and R 1 are any non-interfering group and X is chloro, bromo, iodo, triflates, or nonaflates to amines (primary and secondary). In particular, a process is described for the synthesis of the aminoarylboronic esters via a step-wise or tandem process in which one catalytic event is a metal-catalyzed borylation and the other catalytic event is a metal-catalyzed amination.
专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:US-6048991-A 优先权日:1990-11-16 标题:Preparation of epoxides 发明人:HAERMELING DIETER 权利人:BASF AG 摘要:Alpha-hydroxy-epoxides of alpha-alkoxy-epoxides of the formula IV ##STR1## in which the substituents have the following meanings: R 7 , R 8 , R 9 , R 10 , R 11 are independently hydrogen, C 1 -C 20 -alkyl, C 3 -C 12 -cycloalkyl, C 4 -C 20 -cycloalkylalkyl, C 1 -C 20 -hydroxy-alkyl, a heterocyclic ring, or an aryl or C 7 -C 20 -arylalkyl group optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen, C 1 -C 4 -haloalkyl, C 1 -C 4 -halo-alkoxy, phenyl, phenoxy, halophenyl, halophenoxy, carboxy, C 2 -C 8 -alkoxycarbonyl, or cyano, or R 7 and R 8 or R 7 and R 9 or R 7 and R 10 or R 9 and R 10 or R 10 and R 11 together form a (CH 2 ) n group in which n is an integer from 1 to 10 and which may be optionally substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, and/or halogen, and n R 12 is hydrogen, C 1 -C 8 -alkyl, or benzyl, n provided that R 10 is not hydrogen, methyl, ethyl, propyl, or cyclohexyl when R 7 , R 8 , R 9 , or R 11 is hydrogen, that R 7 is not methyl when R 8 is methyl or phenyl and R 9 , R 10 , or R 11 is hydrogen, that R 7 is not methyl when R 8 , R 9 , R 10 , or R 11 is hydrogen and R 12 is ethyl, that R 7 is not phenyl or hexyl when R 8 , R 9 , R 10 , or R 11 is hydrogen, that R 9 is not methyl when R 7 , R 8 , R 10 , or R 11 is hydrogen, that R 10 and R 11 are not methyl when R 7 , R 8 , or R 9 is hydrogen, and that R 7 and R 10 do not together form an unsubstituted cycloalkyl when R 8 , R 9 , or R 11 is hydrogen. The epoxides of the above formula serve as intermediates for the synthesis of, inter alia, perfumes, plant protectants and polymers.
专利号:WO-0021917-A1 优先权日:1998-10-13 标题 :Pharmaceutical intermediate for the synthesis of fluoxetine and a process for the preparation thereof 发明人:REITER JOZSEFNE; SIMIG GYULA; MEZEI TIBOR; IMRE JANOS; VERECZKEYNE DONATH GYOERGYI; NAGY KALMAN; NEMETH NORBERT; SZABO TIBOR 权利人:EGYT GYOGYSZERVEGYESZETI GYAR; REITER JOZSEFNE; SIMIG GYULA; MEZEI TIBOR; IMRE JANOS; VERECZKEYNE DONATH GYOERGYI; NAGY KALMAN; NEMETH NORBERT; SZABO TIBOR 摘要:The invention relates to N,N-dimethyl-{3-phenyl-3-[(4-trifluoromethyl)-phenoxy]-propyl-amine}-p-toluenesulfonate of Formula (I) and an improved process for the preparation thereof. The new compound of Formula (I) is a valuable pharmaceutical intermediate useful in the preparation of the antidepressant having the generic name fluoxetine.
专利号:US-2016073631-A1 优先权日:2013-03-04 标 题 :Process for the preparation of dihydropyrrole derivatives 发明人:EL QACEMI MYRIEM; SMITS HELMARS; CASSAYRE JEROME YVES; MULHOLLAND NICHOLAS PHILLIP; RENOLD PETER; GODINEAU EDOUARD; PITTERNA THOMAS 权利人:SYNGENTA PARTICIPATIONS AG; SYNGENTA LTD 摘要:The present invention provides stereoselective processes for the preparation of compounds of formula (I) n n n n n n n n n n n n wherein n P is phenyl, naphthyl, a 6-membered heteroaryl group containing one or two nitrogen atoms as ring members, or a 10-membered bicyclic heteroaryl group containing one or two nitrogen atoms as ring members, and wherein the phenyl, naphthyl and heteroaryl groups are optionally substituted; n R 1 is chlorodifluoromethyl or trifluoromethyl; n R 2 is optionally substituted aryl or optionally substituted heteroaryl; n n is 0 or 1; n including the process comprising n (a-i) reacting a compound of formula II n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; n with nitromethane in the presence a chiral catalyst to give a compound of formula III n n n n n n n n n n n n n n n n wherein P, R 1 and R 2 are as defined for the compound of formula I; and n (a-ii) reductively cyclising the compound of formula III to give the compound of formula I. n n n n n The invention also provides intermediates useful for processes for the synthesis of compounds of formula (I).
专利号:US-8114993-B2 优先权日:2007-02-06 标题:Use of aryl chlorides in palladium-catalyzed C-H bond functionalization 发明人:DAUGULIS OLAFS; CHIONG HENDRICH 权利人:DAUGULIS OLAFS; CHIONG HENDRICH; UNIV HOUSTON SYSTEM 摘要:A one-step method for efficiently converting carbon-hydrogen bonds into carbon-carbon bonds using chloroarenes and palladium catalysts is disclosed. This method allows faster introduction of complex molecular entities, a process that would otherwise require many more steps. This invention is particularly relevant for the organic synthesis of complex molecules such as, but not limited to, pharmacophores.
摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 141. 摘要:Marsden, S. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 586. 摘要:Neumann, H.; Schranck, J., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 68. 摘要:Ouali, A.; Taillefer, M., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 97. 摘要:Elie, M.; Renaud, J.-L.; Gaillard, S., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 1, 231.