CAS: 403-54-3; 3-Fluorobenzonitrile

上下游产品

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3-氯苯腈置于四甲基氟化铵体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 24.0H,以7%的收率获得产物3-氟苯腈
参考文献:室温s N Ar氟化的无水四甲基氟化铵
标题:室温s N Ar氟化的无水四甲基氟化铵
摘要:本文介绍了使用无水四甲基氟化铵(nme 4 F)在室温下对芳基卤化物和硝基芳烃进行s N Ar氟化.该试剂在温和的条件下(通常在室温下)有效地将芳基-X(x = Cl,Br,I,No 2,Otf)转化为芳基-F.该反应的底物包括缺电子的杂芳族化合物(22个实例)和芳烃(5个实例).反应的相对速率随x以及底物的结构而变化.但是,一般而言,带有x = No 2的基材或br反应最快.在所检查的所有情况下,这些反应的产率均与在升高的温度(即,更传统的卤代氟化条件)下使用csf所获得的产率相当或更好.反应还提供了可比较的产量,规模从100 Mg到10 G不等.进行了成本分析,结果表明,使用nme 4 F进行氟化处理通常比使用csf进行氟化处理更具成本效益.
DOI:10.1021/acs.Joc.5B02075

专利信息

专利号:US-4822903-A
优先权日:1981-05-15
标题:Fluorinated silica catalyst and preparation of aromatic/aliphatic nitriles in the presence thereof
发明人：JACQUES ROLAND; REPPELIN MICHEL; SEIGNEURIN LAURENT
权利人:RHONE POULENC SPEC CHIM
摘要:An improved fluorinated siliceous catalyst, well adapted for the catalytic synthesis of aromatic/aliphatic nitriles from their corresponding formamides, formanilides or amides, is comprised of a plurality of silica particulates, the specific surface of which ranging from about 200 to about 300 m 2 /g, having a total pore volume ranging from about 1 to about 1.5 cm 3 /g, with an average pore diameter ranging from about 100 to about 200 â„«, having an exchange pH of less than about 3, and with the fluorine content thereof bonded to the silica, expressed in F 31 , ranging from about 0.05 to about 2% by weight based upon the silica, and the sodium content thereof, expressed as Na 2 O, being less than about 1% by weight, also based upon the silica.

专利号:WO-03080621-A1
优先权日:2002-03-19
标题:Process and intermediates to substituted imidazopyrimidines
发明人：LI WENJIE; CAI DONGWEI; HOERRNER R SCOTT; JENSEN MARK S; LARSEN ROBERT D; PETASIS NICOS A
权利人:MERCK & CO INC; LI WENJIE; CAI DONGWEI; HOERRNER R SCOTT; JENSEN MARK S; LARSEN ROBERT D; PETASIS NICOS A
摘要:A novel process is provided for the preparation of imidazo[1,2-α]pyrimidines which are substituted at the 3-position with a substituted chlorophenyl group. Such compounds are useful in the synthesis of GABAA receptor ligands for the treatment of deleterious mental disorders. Also provided are intermediates obtained from the process useful in the synthesis of GABAA receptor ligands.

专利号:US-6232318-B1
优先权日:1998-11-12
标 题:Pyrimidinedione derivatives useful as alpha 1A adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G
权利人:MERCK & CO LTD
摘要:Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

专利号:WO-0027817-A1
优先权日:1998-11-10
标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G
权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G
摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered uring flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

专利号:WO-0027827-A1
优先权日:1998-11-10
标题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA
权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA
摘要:Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

专利号:US-7754188-B2
优先权日:2003-06-30
标 题:Radiolabeled cannabinoid-1 receptor modulators
发明人：BURNS H DONALD; CHEN ALEX M; GIBSON RAYMOND E; GOULET MARK T; HAGMANN WILLIAM K; HAMILL TERENCE G; JEWELL JAMES P; LIN LINUS S; LIU PING; PERESYPKIN ANDREY V
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.