CAS: 57381-39-2; 2-Bromo-5-Fluorobenzonitrile

该化合物是有机化合物,其特点是苯环上存在溴和氟替代物,以及一个硝三烯功能组,其分子结构包括一个含有溴原子的苯环,第二个位置是溴原子,第五位置是氟原子,而西洋组(-CN)在第一个位置与苯相连,该化合物一般在室温下是固体,并因其在有机合成中的用途而闻名,特别是在制药和农用化学物的开发方面,由于存在电离性卤素和硝三烯组,该物质会影响其再活性和溶性,此外,2-Bromo-5-氟-苯三烯可参与核糖替代反应,并可作为更复杂的化学结构的建筑块.在处理该化合物时,应注意安全防范措施,因为它可能构成卤化有机化合物的典型健康危害.

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CAS号403-54-3 3-氟苯甲腈 | CAS号461451-63-8 2-氰基-4-氟苯硼酸频哪醇酯 | CAS号747392-34-3 2-溴-5-氟苄胺 | CAS号1006-33-3 2'-溴-5'-氟苯乙酮 | CAS号138642-47-4 2-溴-5-甲氧基苯甲腈

合成工艺路线路线简述

    📜3-氟苯腈置于1,3-二溴-5,5-二甲基海因,硫酸体系中,用 乙腈 作为反应溶剂,化学反应 8.0H,以90%的收率获得产物2-溴-5-氟苯腈
    参考文献:Facile Synthesis Of 2-Bromo-3-Fluorobenzonitrile: An Application And Study Of The Halodeboronation Of Aryl Boronic Acids
    标题:Facile Synthesis Of 2-Bromo-3-Fluorobenzonitrile: An Application And Study Of The Halodeboronation Of Aryl Boronic Acids
    摘要:A Scaleable Synthesis Of 2-Bromo-3-Fluorobenzonitrile Via The Naome-Catalyzed Bromodeboronation Of 2-Cyano-6-Fluorophenylboronic Acid Was Developed. The Generality Of This Transformation Was Demonstrated Through The Halodeboronation Of A Series Of Aryl Boronic Acids. Both Aryl Bromides And Aryl Chlorides Were Formed In Good To Excellent Yields When The Corresponding Aryl Boronic Acid Was Treated With 1,3-Dihalo-5,5-Dimethylhydantoin And 5 Mol % Naome.
    DOI:10.1021/jo035184P

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    专利信息


    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-6228870-B1
    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
    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 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-6235759-B1
    优先权日:1998-10-29
    标 题 :Dihydropyridinones and pyrrolinones useful as alpha 1A adrenoceptor antagonists
    发明人:BARROW JAMES C; NANTERMENT PHILIPPE G; SELNICK HAROLD G
    权利人:MERCK & CO INC
    摘要:Novel dihydropyridinone and pyrrolinone 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-6319932-B1
    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
    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:RU-2440355-C2
    优先权日:2006-04-03
    标 题:Method for synthesis of organoelement compounds

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    合成参考文献


    参考文献:10.1055/s-0036-1588303
    摘要:Rossi R, Bellina F, Lessi M, Manzini C, Marianetti G. Direct (Hetero)arylation Reactions of (Hetero)arenes as Tools for the Step- and Atom-Economical Synthesis of Biologically Active Unnatural Compounds Including Pharmaceutical Targets. Synthesis. 2016 Oct 11;48(22):3821–62. doi: 10.1055/s-0036-1588303.
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