📜氰乙酸置于1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,以46%的收率获得产物2-氰基乙酰苯胺 参考文献:Discovery,Structure-Activity Relationship Study And Biological Evaluation Of 2-Thioureidothiophene-3-Carboxylates As A Novel Class Of C-X-C Chemokine Receptor 2 (Cxcr2) Antagonists 标题:Discovery,Structure-Activity Relationship Study And Biological Evaluation Of 2-Thioureidothiophene-3-Carboxylates As A Novel Class Of C-X-C Chemokine Receptor 2 (Cxcr2) Antagonists 摘要:The C-X-C Motif Ligand 8 And C-X-C Chemokine Receptor 2 (Cxcl8-Cxcr2) Axis Is Involved In Pathogenesis Of Various Diseases Including Inflammation And Cancers. Various Cxcr2 Antagonists Are Under Development For Several Diseases. Our Previous High-Throughput Cell-Based Assay Specific For Cxcr2 Has Identified A Pyrimidine-Based Compound Cx797 Acting On Cxcr2 Down-Stream Signaling. A Lead Optimization Campaign Through Scaffold-Hopping Strategy Led To A Series Of 2-Thioureidothiophene-3-Carboxylates (Tutp) As Novel Cxcr2 Antagonists. Structure-Activity Relationship Study Of Tutps Led To The Identification Of Compound 52 That Significantly Inhibited Cxcr2-Mediated Beta-Arrestin Recruitment Signaling (Ic50 = 1.1 +/-0.01 Mu M) With Negligible Effect On Cxcl8-Mediated Camp Signaling And Calcium Flux. Similar To The Known Cxcr2 Antagonist Sb265610,Compound 52 Inhibited Cxcl8-Cxcr2 Induced Phosphorylation Of Erk1/2. Tutp Compounds Also Inhibited Cxcl8-Mediated Cell Migration And Showed Synergy With Doxorubicin In Ovarian Cancer Cells,Thereby Supporting Tutps As Promising Compounds For Cancer Treatment. (C) 2020 Elsevier Masson Sas. All Rights Reserved. DOI:10.1016/j.Ejmech.2020.112387
专利号:WO-0031040-A1 优先权日:1998-11-23 标 题 :Process for preparing bis n-substituted perylenetetra carboximides via bis (hydroxymethyl) perylenetetra carboximide 发明人:HENDI SHIVAKUMAR BASALINGAPPA 权利人:CIBA SC HOLDING AG 摘要:Process for preparing a bis (hydroxymethyl) perylenetetra carboximide compound by reacting perylene-3,4,9,10-tetracarboximide with formaldehyde. The bis (hydroxymethyl) perylenetetra carboximide can be isolated or further reacted in a one pot synthesis to yield a compound of formula (I), wherein X1 and X2, each independently of the other, are organic radicals, D is chlorine or bromine, and n is an integer from 0 to 4; which perylene derivative contains from 0 to 6 moles of -SO3M per mole of the perylene derivative; wherein M is hydrogen or a metal or ammonium cation.
专利号:US-5919945-A 优先权日:1996-06-05 标题 :Process for preparing diketopyrrolopyrrole derivatives 发明人:HENDI SHIVAKUMAR BASALINGAPPA 权利人:CIBA SC HOLDING AG 摘要:This disclosure relates to a process for preparing bis(hydroxymethyl)pyrrolopyrrole compounds of the formula wherein A1 and A2 are aryl radicals, by reacting a 1,4-diketopyrrolopyrrole with formaldehyde. The compound of formula (II) can be isolated or further reacted in a one pot synthesis to yield a compound of the formula wherein B1 and B2 are organic radicals.
专利号:US-6441174-B1 优先权日:1998-11-23 标题:Process for preparing bis(hydroxymethyl)perylenetetracarboximide 发明人:HENDI SHIVAKUMAR BASALINGAPPA 权利人:CIBA SC HOLDING AG 摘要:The invention is directed to a process for preparing a bis(hydroxymethyl)perylenetetracarboximide compound by reacting perylene-3,4,9,10-tetracarboximide with formaldehyde. The bis(hydroxymethyl)perylenetetracarboximide can be isolated or further reacted in a one pot synthesis to yield a compound of the formulawherein X1 and X2 are organic radicals.
专利号:US-4644010-A 优先权日:1982-09-28 标题:Certain β-oxo-α-carbamoylpyrrolepropionitriles 发明人:WALKER GORDON N 权利人:CIBA GEIGY CORP 摘要:1-Unsubstituted β-oxo-α-(phenylcarbamoyl)-β-pyrrolylpropionitriles, e.g. those of the formula ##STR1## wherein R 1 and R 2 =H or alkyl, and R 3 and R 4 =H, alkyl, alkoxy, OH, halogen or CF 3 , are analgesic, and antiarthritic agents. Their synthesis, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds are included.
参考标题:Water/alkali-Catalyzed Reactions Of Azides With 2-Cyanothioacetamides. Eco-Friendly Synthesis Of Monocyclic And Bicyclic 1,2,3-Thiadiazole-4-Carbimidamides And 5-Amino-1,2,3-Triazole-4-Carbothioamides 作者:Valeriy O. Filimonov,Lidia N. Dianova,Tetyana V. Beryozkina,Dmitrii Mazur,Nikolai A. Beliaev,Natalia N. Volkova,Vladimir G. Ilkin,Wim Dehaen,Albert T. Lebedev,Vasiliy A. Bakulev |发布日期:2019.11.1 摘要:Extended To The One-Pot Reaction Of Sulfonyl Chlorides And 6-Chloropyrimidines 2'O With Sodium Azide, Leading To Final Products In Higher Yields, That Is, Avoiding The Isolation Of Unsafe Sulfonyl Azides. The Method Was Furthermore Applied To The Reaction Of N,N'-Bis-(2-Cyanothiocarbonyl)Pyrazine 1H With Sulfonyl Azides To Afford Bicyclic 1,2,3-Thiadiazoles 8 And 1,2,3-Triazoles 9 Connected Via A 1,1'-Piperazinyl
合成参考文献
摘要:Wang, Z.; Shi, T.; Zhang, H.-H., Science of Synthesis Knowledge Updates, (2020) 3, 413. 摘要:Kwiatkowska, M.; Kiełbasiński, P., Science of Synthesis: Knowledge Updates, (2024) 3, 443.