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cyclopropanecarboxylic acid chloride cyclopropanecarboxylic acid bis(trichloromethyl) carbonate Cyclopropylamine1-cyclopropyl-3-phenylurea 1-Cyclopropyl-3-(4-fluorphenyl)-harnstoff 2,3-dihydro-5-(3',4'-dichlorophenyl)-6,7-bis(hydroxymethyl)-1H-pyrrolizine bis(cyclopropylcarbamate) (1S,3S,4S,5R,6R,7R)-1-((4S,5R)-4-Acetoxy-5-methyl-3-methylene-6-phenyl-hexyl)-6-cyclopropylcarbamoyloxy-4-hydroxy-7-(1-methoxy-1-methyl-ethoxy)-2,8-dioxa-bicyclo[3.2.1]°Ctane-3,4,5-tricarboxylic acid tri-tert-butyl ester 环丙甲酸置于4-二甲氨基吡啶,1,1,1-Trichloro-2-Methylpropan-2-Yl Azidoformate体系中,用 乙腈 作为反应溶剂,化学反应生成 异氰酰基环丙烷
参考文献:使用 1,1-二甲基-2,2,2-三氯乙氧基羰基叠氮化物的 Dmap 催化一锅 Curtius 重排
标题:使用 1,1-二甲基-2,2,2-三氯乙氧基羰基叠氮化物的 Dmap 催化一锅 Curtius 重排
摘要:我们报告了使用 1,1-二甲基-2,2,2-三氯乙氧基羰基叠氮化物 (Dmtn 3) 和 4-(二甲氨基)吡啶 (Dmap) 作为催化剂开发的可控,无碱,一锅 Curtius 重排.该催化过程的范围涵盖一系列伯,仲和叔烷基和芳基羧酸,可实现烷基或芳基异氰酸酯的有效立体有择构造.报道了天然产物和药物分子的后期脱羧异氰化,几种药物的快速合成以及原位反应生成的 Dmtn 3的利用的例子.对该机理的详细研究表明,反应速率取决于dmap催化剂的浓度,这确保了反应是一个温和且可控的过程.
DOI:10.1021/acs.Orglett.3C01580
专利信息
专利号:US-12247037-B2
优先权日:2018-12-12
标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders
发明人:BRANDT GARY
权利人:NEUMORA THERAPEUTICS INC
摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
专利号:US-4505792-A
优先权日:1981-03-03
标题:Photochemical rearrangement of 2-aminopyrrolin-5-ones to aminocyclopropyl isocyanates and polymers thereof
发明人:KOCH TAD H; SWANSON BARRY J
权利人:UNIVERSITY PATENTS INC
摘要:Subjecting 1,4-bis-[(pyrrolin-3-onyl)methylamino]-2-butyne to ultraviolet irradiation effects rearrangement in greater than 80% yield to 1,4-bis-[(isocyanatocyclopropyl)methylamino]-2-butyne. The diisocyanate is useful in the synthesis of polyurethanes and polyureas and also for the in situ photochemical generation of a cross-linking agent for polyurethanes and structurally related polymers.
专利号:US-4380647-A
优先权日:1981-03-03
标 题 :2-Aminopyrrolin 5-ones and aminocyclopropyl isocyanates therefrom
发明人:KOCH TAD H; SWANSON BARRY J
权利人:UNIVERSITY PATENTS INC
摘要:Subjecting 1,4-bis-[(pyrrolin-3-onyl)methylamino]-2-butyne to ultraviolet irradiation effects rearrangement in greater than 80% yield to 1,4-bis-[(isocyanatocycloprolpyl)methylamino]-2-butyne. The diisocyanate is useful in the synthesis of polyurethanes and polyureas and also for the in situ photochemical generation of a cross-linking agent for polyurethanes and structurally related polymers.
专利号:CN-104341482-A
优先权日:2013-08-09
标 题 :Synthesis of a Heterocyclic Sulfonic Acid Derivative and Its Application in Drug Therapy
专利号:CN-104341482-B
优先权日:2013-08-09
标题 :Synthesis of a Heterocyclic Sulfonic Acid Derivative and Its Application in Drug Therapy
专利号:US-2011015119-A1
优先权日:2009-06-24
标题:Novel semi-synthetic glycopeptides as antibacterial agents
发明人:CHU DANIEL; YE TAO; WANG BING
权利人:LEAD THERAPEUTICS INC
摘要:Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.