合成目标产物 4-(1H-Imidazol-1-yl)Benzaldehyde 主要起始原料 Imidazole And 4-Iodobenzaldehyde
(文献来源)合成步骤主要原料 Imidazole 和 4-Iodobenzaldehyde
4-(1-咪唑基)苯甲酸乙酯置于sodium Tetrahydroborate,Pyridinium Chlorochromate,Calcium Chloride体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应 1.5H,反应生成1-(4-甲醛基苯基)咪唑 参考文献:Aromatic Hydrazides As Specific Inhibitors Of Bovine Serum Amine Oxidase 标题:Aromatic Hydrazides As Specific Inhibitors Of Bovine Serum Amine Oxidase 摘要:New Hydrazides Were Synthesized In Search For Specific Inhibitors Of Bovine Serum Amine Oxidase: A Series Of Benzoic And Phenylacetic Acid Hydrazides Containing The 1H-Imidazol-1-Yl Or The 1H-Imidazol-1-Ylmethyl Group As (O,M,P)-Substituent In The Phenyl Ring; An Analogous Series Of P-Substituted Phenylhydrazides With 5 Or 6-Membered Heterocyclic Ring As Substituent,And A Series Of Similar Phenylpropionic Hydrazides. The Longer And More Flexible Phenylacetic Hydrazides,And To A Somewhat Lesser Extent The Phenylpropionic Ones,Were Better Specific Inhibitors Of Bovine Serum Amine Oxidase Than The Benzoic Hydrazides,Which Were Also Bound By The Enzyme With High Affinity,But At A Slow Rate. Derivatives With P-And M-Substituents Were More Reactive Than The O-Substituted Ones. The Chemical Nature Of The Substituent Was Less Important Than Its Position In The Phenyl Ring And The Presence Of Methylene Spacers. These Data Point To The Presence Of A Hydrophobic Site At Short Distance From The Protein Carbonyl Cofactor,So That Simultaneous Interaction Of The 2 Ends Of The Inhibitor Molecule Can occur At The 2 Sites. The Presence Of The Hydrophobic Site Was Confirmed By The Capability Of Some Molecule Deprived Of The Hydrazidic Group To Act As Mild Inhibitors. All Hydrazides Were Less Reactive By 2-3 Orders Of Magnitude Towards Pig Kidney Diamine Oxidase And Fad-Dependent Monoamine Oxidase From Rat Brain Mitochondria,While The Other Compounds Showed Similar Inhibition Power Against All Proteins. The Specificity For The Bovine Enzyme Seems Therefore To Be Related To The Concerted Action Of The 2 Moieties Of The Inhibitor Molecule. Doi:10.1016/0223-5234(92)90005-L
专利信息
专利号:US-5246957-A 优先权日:1991-04-24 标题 :N-imidazolyl derivatives of substituted indole 发明人:COZZI PAOLO; PILLAN ANTONIO; PULICI MAURIZIO; SALVATI PATRICIA; VOLPI ANGELO D 权利人:ERBA CARLO SPA 摘要:The invention provides N-imidazolyl derivatives of substituted indole of general formula (I) ##STR1## wherein p is an integer of 1 to 4; n A is a straight or branched C 1 -C 4 alkylene chain; n B is a direct linkage, a straight or branched, unsaturated or saturated C 1 -C 4 hydrocarbon chain; n Q is a straight or branched, saturated or unsaturated C 1 -C 9 hydrocarbon chain, or said chain is interrupted by an oxygen atom; n each of R 1 and R 2 independently is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfonyl, halogen or trihalomethyl; n each of R 3 and R 5 , independently, is hydrogen or C 1 -C 4 alkyl; n R 4 is a --OR 6 or --N(R 6 R 7 ) group, wherein each of R 6 and R 7 independently is hydrogen, C 1 -C 4 alkyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of a disease state in which an enhancement of TxA 2 synthesis exerts a pathogenic effect.
专利号:US-5238953-A 优先权日:1991-01-22 标题:N-imidazolyl derivatives of substituted tetrahydrocarbazole and cyclohept (b) indole 发明人:COZZI PAOLO; PILLAN ANTONIO; PULICI MAURIZIO; SALVATI PATRICIA; VOLPI ANGELO D 权利人:ERBA CARLO SPA 摘要:The invention provides new N-imidazolyl derivatives of substituted tetrahydrocarbazoles and cyclopent[b]indoles of general formula (I) ##STR1## wherein n is 1 or 2; n p is an integer of 1 to 4; n A is a straight or branched C 1 -C 4 alkylene chain; n B is a direct linkage, a straight or branched, unsaturated or saturated C 1 -C 4 alkylene chain; n Q is a direct linkage or a straight or branched C 1 -C 4 alkylene chain; n each of R 1 and R 2 independently is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulfonyl, halogen or trihalomethyl; n each of R 3 and R 5 , independently is hydrogen or C 1 -C 4 alkyl; n R 4 is --OR 6 or --N(R 6 ,R 7 ) group, wherein each of R 6 and R 7 independently is hydrogen, C 1 -C 4 alkyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of a disease state in which an enhancement of TxA 2 synthesis exerts a pathogenic effect.
[参考文献]: Vijay K Marrapu, Et Al. Novel Aryloxy Azolyl Chalcones With Potent Activity Against Mycobacterium Tuberculosis H37Rv. Eur J Med Chem. 2011 Sep;46(9):4302-10.
合成参考文献
摘要:Ahmad, O. K.; Movassaghi, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 195. 摘要:Liu, G.; Feng, J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 338.