CAS: 2863-98-1; 4-Hydrazinylbenzonitrile Hydrochloride

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CAS号873-74-5 对氨基苯腈 | CAS号33348-34-4 4-氨基-3-碘苯腈 | CAS号144035-34-7 [2-(5-氰基-1H-吲哚-... | CAS号100723-77-1 6,7,8,9-四氢-5H-咔... | CAS号1029691-07-3 2-(1,3-二氧代异吲哚啉-... | CAS号827316-54-1 4-[2-(1-pyrazol... | CAS号628294-80-4 1,2,3,4-tetrahy... | CAS号640727-98-6 1-(4-氰基-苯基)-5-(...

对氨基苯腈置于盐酸,Sodium Hydrogensulfite体系中,用 水 用作溶剂,化学反应 3.5H,反应生成4-氰基苯肼盐酸盐
参考文献:维拉佐酮的合成研究
标题:维拉佐酮的合成研究
摘要:以 4-氰基苯胺和 5-溴-2-羟基苯甲醛为起始原料,描述了一种合成维拉佐酮的新途径,总产率为 24%,纯度为 99%.首先,通过 4-氰基苯胺的重氮化合成中间体 (3-(4-氯丁基)-1H-Indole-5-Carbonitrile),然后用 6-氯己醛进行 Fischer 吲哚环化.随后,通过用哌嗪对 5-溴苯并呋喃-2-甲酰胺进行芳香族亲核取代,生成另一种中间体 5-(哌嗪-1-基) 苯并呋喃-2-甲酰胺.最后,通过用 Et3N/k2Co3 处理上述两个关键中间体的亲核取代获得维拉佐酮.与原始工艺相比,该路线避免了使用昂贵且有毒的试剂,并解决了安全,环境问题和高成本等问题.
Doi:10.1177/1747519819893293

专利信息

专利号:US-8283476-B2
优先权日:2007-06-26
标 题:Transition metal catalyzed synthesis of 2H-indazoles
发明人：HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS
权利人:HALLAND NIS; NAZARE MARC; LINDENSCHMIDT ANDREAS; ALONSO JORGE; RKYEK OMAR; URMANN MATTHIAS; SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.

专利号:US-7211598-B2
优先权日:2002-06-28
标 题:Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; RANATUNGE RAMANI R; RICHARDSON STEWART K
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-7442802-B2
优先权日:2002-06-27
标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-2010234601-A1
优先权日:2007-06-26
标 题 :Transition metal catalyzed synthesis of 2H-indazoles

专利号:WO-2009000411-A1
优先权日:2007-06-26
标 题 :A transition metal catalyzed synthesis of 2h-indazoles

专利号:EP-2170833-A1
优先权日:2007-06-26
标 题 :A transition metal catalyzed synthesis of 2h-indazoles