364-78-3 = 345-17-5 + 80517-21-1 反应条件:1.1 Reagents: Sodium Nitrite,Hydrochloric Acid Solvents: Water1.2 Reagents: Sodium Cyanide,Cuprous Chloride 标题:Fluorinated Tricyclic Neuroleptics With Prolonged Action. 7-Fluoro-11-[4-(2-Hydroxyethyl)Piperazino]-2-Isopropyl-10,11-Dihydrodibenzo[b,F]Thiepin 作者:Protiva,Miroslav; Et Al 参考文献:Collection Of Czechoslovak Chemical Communications 日期:1986 卷标:51(3) 页码:698-722
1-氯-4-氟苯置于硝酸体系中,化学反应生成2-氯-5-氟硝基苯 参考文献:Ingold; Vass,Journal Of The Chemical Society,1928,P. 2265 标题:Ingold; Vass,Journal Of The Chemical Society,1928,P. 2265
专利号:CN-1007150-B 优先权日:1987-06-22 标题 :Synthesis of 2,4-dichlor-5-fluor benzoic acid
专利号:US-6096763-A 优先权日:1995-02-23 标题 :α1a adrenergic receptor antagonists 发明人:HOFFMAN JACOB M; CHANG RAYMOND S L 权利人:MERCK & CO INC 摘要:This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α 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 are achieved.
专利号:WO-9625934-A1 优先权日:1995-02-23 标题 :ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS 发明人:EVANS BEN E; PONTICELLO GERALD S; HOFFMAN JACOB M; CHANG RAYMOND S L 权利人:MERCK & CO INC; EVANS BEN E; PONTICELLO GERALD S; HOFFMAN JACOB M; CHANG RAYMOND S L 摘要:This invention relates to novel compounds, their synthesis and use as selective α1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α1a 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 are achieved.
专利号:US-5952351-A 优先权日:1995-02-23 标题 :Alpha 1a adrenergic receptor antagonists 发明人:EVANS BEN E; PONTICELLO GERALD S; HOFFMAN JACOB M 权利人:MERCK & CO INC 摘要:PCT No. PCT/US96/02534 Sec. 371 Date Aug. 13, 1997 Sec. 102(e) Date Aug. 13, 1997 PCT Filed Feb. 23, 1996 PCT Pub. No. WO96/25934 PCT Pub. Date Aug. 29, 1996This invention relates to novel compounds, their synthesis and use as selective alpha 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The 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 are achieved.
专利号:US-5760054-A 优先权日:1994-04-14 标题:Alpha IC adrenergic receptor antagonists 发明人:HUFF JOEL R; LEE HEE-YOON; NERENBERG JENNIE B; THOMPSON WAYNE J; BELL IAN M 权利人:MERCK & CO INC 摘要:PCT No. PCT/US95/04590 Sec. 371 Date Oct. 1, 1996 Sec. 102(e) Date Oct. 1, 1996 PCT Filed Apr. 13, 1995 PCT Pub. No. WO95/28397 PCT Pub. Date Oct. 26, 1995This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1C adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hypertrophy. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha1C receptor subtype without at the same time inducing orthostatic 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 are achieved.
[参考文献]: Grace G Shiue, Et Al. N,N-Dimethyl-2-(2-Amino-4-(18)F-Fluorophenylthio)-Benzylamine (4-(18)F-Adam): An Improved Pet Radioligand For Serotonin Transporters. J Nucl Med. 2003 Dec;44(12):1890-7.