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2-bromoaniline mesoaldehyde 1,3-dioxime-2-(o-bromophenyl)hydrazone 2-(2-Bromo-phenyl)-1,2-dihydro-phthalazin-1-ol 2-(2-Bromo-phenyl)-3-oxo-3,5-dihydro-2H-pyridazino[4,3-b]indole-4-carboxylic acid 2-(2-Bromo-phenyl)-3-oxo-3,5-dihydro-2H-pyridazino[4,3-b]indole-4-carboxylic acid ethyl ester 合成工艺路线路线简述
- 合成目标产物 2-Bromophenylhydrazine Hydrochloride 主要起始原料 2-Bromoaniline
- (文献来源)合成步骤主要原料 2-Bromoaniline
2-溴苯胺置于盐酸,Sodium Nitrite,Tin(II) Chloride Dihdyrate体系中,用 水 作为反应溶剂,化学反应 3.0H,反应生成 2-溴苯肼盐酸盐
参考文献:作为具有新型结合模式的 Pdhc-E1 抑制剂的 2,6-二甲基-4-氨基嘧啶腙的设计,合成和抗真菌活性
标题:作为具有新型结合模式的 Pdhc-E1 抑制剂的 2,6-二甲基-4-氨基嘧啶腙的设计,合成和抗真菌活性
摘要:一系列新型 2,6-二甲基-4-氨基嘧啶腙5被合理设计和合成为丙酮酸脱氢酶复合物 E1 (Pdhc-E1) 抑制剂.化合物5强烈抑制大肠杆菌(e.Coli)pdhc-E1(ic 50值为 0.94-15.80 μm).分子对接,定点诱变,酶促和抑制动力学分析表明,化合物5竞争性抑制 Pdhc-E1 并以"直线"模式结合在大肠杆菌pdhc-E1 活性位点,这是一种新的结合模式. 在体外抗真菌试验中,大多数化合物5在50μg/ Ml的显示针对六个测试植物病原性真菌,包括菌丝生长超过80%的抑制灰霉病,念珠菌fructigena,炭疽病菌,和葡萄座腔dothidea侵染.值得注意的是,5F和5I对m. Fructigena 的效力是商业杀菌剂克菌丹和百菌清的1.8-380 倍.在体内,与商业杀菌剂戊唑醇相比,5F和5I控制m. Fructigena的生长.因此,5F和5I对防治果蝇桃褐腐病具有潜在的商业价值.
DOI:10.1021/acs.Jafc.0C07701
专利信息
专利号:US-11040938-B2
优先权日:2016-07-27
标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts
发明人:MA BING; PAN SHUAI
权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH
摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:US-6906046-B2
优先权日:2000-12-22
标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes
发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY
权利人:CELLTECH R & D INC
摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-8212056-B2
优先权日:2008-06-30
标 题 :Ligands for transition-metals and methods of use
发明人:KWONG FUK YEE; SO CHAU MING
权利人:KWONG FUK YEE; SO CHAU MING; UNIV HONG KONG POLYTECHNIC
摘要:The present invention relates to indolyl phosphine ligands, and methods of making such ligands utilizing phenyl hydrazines and aryl ketones as the starting material. The present invention further includes uses of the ligands in the synthesis of pharmaceuticals, materials, and agriculture.
专利号:US-6916922-B2
优先权日:2000-11-03
标题 :Process for the preparation of 1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta [B] [1,4] diazepino- [6,7,1-hi] indole derivatives
发明人:CHAN ANITA W-Y
权利人:WYETH CORP
摘要:This invention provides a process for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1,4]diazepino[6,7,1-hi]indole derivatives of the general formula: n n nwherein: R is H, alkyl, cycloalkyl, —CH 2 -cycloalkyl, acyl, aryl or aroyl; R 1 , R 2 , R 4 and R 5 are H, hydroxy, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO 2 -alkyl, —SO 2 —NH-alkyl, alkyl amide, amino, alkylamino, dialkylmino, fluorinated alkoxy, acyl, aryl or aroyl; R 3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, alkyl sulfonamide, alkyl amide, amino, alkylamino, dialkylmino, fluorinated alkoxy, acyl, aryl or aroyl; or a pharmaceutically acceptable salt thereof, as well as intermediates for their synthesis.
专利号:US-11453670-B2
优先权日:2018-06-11
标 题:Substituted heterocycle fused gamma-carbolines synthesis
发明人:LI PENG; ZHANG QIANG
权利人:INTRA CELLULAR THERAPIES INC
摘要:The present invention provides improved methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.
专利号:CN-110831941-A
优先权日:2018-06-11
标 题 :Synthesis of substituted heterocycle fused gamma-carboline compound