CAS: 133690-91-2; 2-[4-(Azidomethyl)Phenyl]Benzonitrile

相似化合物

1924-77-2 893736-75-9 133690-92-3

上下游产品

4'-(bromomethyl)-1,1'-biphenyl-2-carbonitrile 2-Cyano-4'-methylbiphenyl water [(2'-cyanobiphenyl-4-yl)methyl]amine -2,4-dihydro-2-(2,2-dimethyl-1-propyl)-3H-1,2,4-triazol-3-one5-n-butyl-4-(2'-cyanobiphenyl-4-yl)methyl-2,4-dihydro-2-(2,2-dimethyl-1-propyl)-3H-1,2,4-triazol-3-one 4'-[3-Butyl-1-(2-hydroxy-1-methyl-ethyl)-5-oxo-1,5-dihydro-[1,2,4]triazol-4-ylmethyl]-biphenyl-2-carbonitrile -3H-1,2,4-triazol-3-one2,5-dibutyl-2,4-dihydro-4-(2-cyano-1,1'-biphenyl-4'-yl)methyl-3H-1,2,4-triazol-3-one

📜2-氰基-4'-甲基联苯置于n-溴代丁二酰亚胺(Nbs),Sodium Azide,偶氮二异丁腈体系中,用 四氯化碳,N,N-二甲基甲酰胺 用作溶剂,化学反应 24.0H,反应生成厄贝沙坦杂质19
参考文献:Synthesis And Structure-Activity Relationships Of Nonpeptide,Potent Triazolone-Based Angiotensin Ii Receptor Antagonists
标题:Synthesis And Structure-Activity Relationships Of Nonpeptide,Potent Triazolone-Based Angiotensin Ii Receptor Antagonists
摘要:2,5-Dibutyl-2,4-Dihydro-4-[[2-(1H-Tetrazol-5-yl)[1,1'-Biphenyl]-4'-Yl]Methyl]-3H-1,2,4-Triazol-3-One,Sc-51316,Was Synthesized As A Potent And Orally Active Angiotensin Ii (Aii) Receptor Antagonist With A Long Duration Of Action. To Explore The Lipophilic Pocket In The Aii Receptor Interacting With The Substituent At The 2-Position Of Triazolone-Based Antagonists,A Series Of Compounds Were Prepared And Evaluated For Receptor Binding Affinity And Antagonism Of Aii-Contracted Rabbit Aortic Rings. It Has Been Found That The Pocket Is Very Spacious And Can Accommodate Different Sizes Of Lipophilic Groups And Various Functionalities. Acidic Groups Generally Result In A Slight Decrease In Binding Affinity. Branched Chains Are Unfavorable. The Freedom Of Rotation Around C2-C3 In The Flexible Side Chain Is Crucial For Good Binding. The 2-Phenylethyl-Substituted Triazolone Analogue Exhibits The Highest In Vitro Potency Among All Compounds That Have Been Synthesized.
Doi:10.1021/jm00067A015

专利信息

专利号:WO-2023046836-A1
优先权日:2021-09-24
标 题:Process for preparing sartans
发明人：ZUPANCIC SILVO; SENICAR TANJA; PERÅ E BOÅ TJAN; BOMBEK SERGEJA; KLOBCAR ANDREJ; KRAÅ OVEC DuÅ¡an
权利人:KRKA D D NOVO MESTO
摘要:The present application relates to a process for purifying a tetrazole-containing-sartan or a tetrazole-containing-sartan intermediate, the process comprising the steps of (a) providing a composition comprising an azide-impurity together with a tetrazole-containing-sartan or with an intermediate of a tetrazole-containing-sartan; (b) treating the composition provided in step (a) with a reducing agent; preferably reacting the azide-impurity with a reducing agent thereby obtaining an amine-impurity; and (c) optionally, isolating the tetrazole-containing-sartan or the intermediate of the tetrazole-containing-sartan from the composition. The application further relates to a process for the synthesis of tetrazole-containing-sartans which ensures azide-impurities free final active pharmaceutical ingredients as well as azide-impurities free intermediates of tetrazole-containing-sartans that are suitable for the subsequent synthesis of tetrazole-containing-sartans.

专利号:CN-112415107-A
优先权日:2021-01-21
标 题 :A kind of detection method of impurities in the synthesis of sartans drugs

专利号:CN-112415107-B
优先权日:2021-01-21
标 题 :A method for detecting impurities in the synthesis of sartan drugs