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4个新型有机磷缩合试剂的合成及其在生物活性肽合成中… 总被引:1,自引:0,他引:1
报道了4个新型有机磷化合物:N-二乙氧基磷酰并恶唑酮(DEPBO0,N-(2-氧-1,3,2-二氧杂磷环己烷基)-苯并恶唑酮(DOPBO),3-(2′-氧-1′,3′,2′-二氧杂磷杂环己烷基)-氧-1,2,3-苯并三嗪-4(3H)-酮()DOPBT)和3-(二乙氧基磷酰基)-氧-1,2,3-苯并三嗪-4(3H)-酮(DEPBT)的合成,并研究了它们作为缩合试剂的多肽合成中的应用,研究结果表明,它 相似文献
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建立了利托那韦的合成新方法。N-{N-甲基-N-[(2-异丙基-4-噻唑基)甲基]氨基羰基}-L-缬氨酸(1)与(2S,3S,5S)-5-氨基-2-{N-[(5-噻唑基)-甲氧羰基]氨基}-1,6-二苯基-3-羟基己烷在3-(二乙氧基磷酰氧基)-1,2,3-苯并三嗪-4-酮催化下于室温经缩合反应合成了利托那韦,其结构经1H NMR,13C NMR,MS和元素分析确证。在最佳反应条件[1 0.2 mol,DEPBT 0.25 mmol,二氯甲烷为溶剂,三乙胺为缚酸剂,于室温反应过夜]下,收率72.6%。 相似文献
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当用DEPBT作为缩合试剂合成含组氨酸的肌肽(β-Ala-His)衍生物时, 又偶然发现了另一个副反应. 在这个反应中, 没有得到预期的肌肽产物, 而是生成了一个结构与DEPBT相关的副产物EODhbt(3-乙氧基-3,4-二氢-1,2,3-苯并三嗪-4-酮). 本文报道了此副产物的发现、 结构鉴定及影响副反应的各种因素. 这对深入了解DEPBT的反应特性, 并且在含组氨酸的多肽合成中更有效地应用DEPBT提供了有用的信息. 相似文献
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以2-溴甲基-6,7-亚甲二氧基-3-喹啉酸乙酯(1)为原料,经三步合成了2-叔丁基-4-氟-苯并氧杂卓并[3,4-b]喹啉并[9,11]二氧戊环-14(6H)-酮(4)。其中,6-(2-氟-4-叔丁基-苯氧甲基)-[1,3]二氧戊环并[4,5-g]喹啉-7-羧酸是经一锅法合成的。它的分子内闭环反应是在Eaton’s reagent(P2O5-CH3SO3H)的作用下,在较温和的条件下进行的。所得新化合物3和4的结构经IR1、H NMR和元素分析得以证实。 相似文献
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三类杉酯碱是一种具有显著抗肿瘤活性的化合物, 在以磷脱基, 磺酰基乙酰基作N-苯乙基甘氨酸上氨基的保护基进行分子内酰化的Friede-Crafts反应, 合成三尖杉酯碱母核-(N-7,8-亚甲二氧苯并-3-氮杂环庚酮-1)时所得结果相差甚远, 特别是用磷酰基保护甘氨酸衍生物可以避免脱羰, 顺利地进行内酰化反应, 对合成三尖杉酯碱的母核有重要的意义。为了阐明磷酰基对氨基酸中氮原子上的弧对电子的稳定作用, 我们测定了N-二异丙基磷酰基-N-[2-(3',4'-亚甲二氧苯基)]乙基甘氨酸的单晶结构。 相似文献
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三类杉酯碱是一种具有显著抗肿瘤活性的化合物, 在以磷脱基, 磺酰基乙酰基作N-苯乙基甘氨酸上氨基的保护基进行分子内酰化的Friede-Crafts反应, 合成三尖杉酯碱母核-(N-7,8-亚甲二氧苯并-3-氮杂环庚酮-1)时所得结果相差甚远, 特别是用磷酰基保护甘氨酸衍生物可以避免脱羰, 顺利地进行内酰化反应, 对合成三尖杉酯碱的母核有重要的意义。为了阐明磷酰基对氨基酸中氮原子上的弧对电子的稳定作用, 我们测定了N-二异丙基磷酰基-N-[2-(3',4'-亚甲二氧苯基)]乙基甘氨酸的单晶结构。 相似文献
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稀土配合物的研究 IV: 稀土元素与4-酰代双吡唑啉酮BPMPPD及1,10-二氮杂菲三元配合物的合成和性质的研究 总被引:1,自引:0,他引:1
4-酰代双吡唑啉酮是一类新型β双酮多啮金属离子螯合剂和萃取剂, 其性能优于单吡唑啉酮, 本文继合成1,5-双(1'-萃基-3'-甲基-5'-氧代吡唑-4')-1,5-戊二酮(BPMPPD, H2A)后, 又合成了它和1,10-二氮杂菲(Phen, P)与稀土元素形成的三元固态配合物, 并对这些新配合物的性质进行了研究。 相似文献
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4-酰代双吡唑啉酮是一类新型β双酮多啮金属离子螯合剂和萃取剂, 其性能优于单吡唑啉酮, 本文继合成1,5-双(1'-萃基-3'-甲基-5'-氧代吡唑-4')-1,5-戊二酮(BPMPPD, H2A)后, 又合成了它和1,10-二氮杂菲(Phen, P)与稀土元素形成的三元固态配合物, 并对这些新配合物的性质进行了研究。 相似文献
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A cycloheptapeptide cyclo(Gly-Tyr-Gly-Gly-Pro-Phe-Pro), which was isolated and identified from one kind of Chinese medicinal herbs, was chosen as a model cyclopeptide, to evaluate an organophosphorus reagent, 3-(diethyloxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one(DEPBT) for synthesis of cyclopeptide and compared with two other organophosphorus reagents, DPPA and BOP. 相似文献
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[formula: see text] The new crystalline phosphate reagent 3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one (DEPBT) mediates amide bond formation with a remarkable resistance to racemization. Comparative racemization studies were carried out and DEPBT proved to be superior to typical phosphonium and uronium coupling reagents. DEPBT is easily prepared and is exceedingly stable with a shelf life of months at room temperature. The advantageous properties of DEPBT render it a useful and unique addition to the arsenal of coupling reagents. 相似文献
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3- (Diethoxyphosphoryloxy)- 1,2,3-benzotriazln-4 (3H)-one (DE-PBT) was an organophosphorus coupling reagent developed by our group. It was an effective coupling reagent for the synthesis of protected peptides containing Tyr, Ser and Thr with unprotected hydroxy group on their side chain. The further study of the synthesis of a series of protected dipeptides containing hisfidine with unprotected imidazole group using DEPBT is reported. During the synthetic procedure, the imidazole group of histidine did not need to be protected. When the carboxyl components were N-protected aromatic amino acids or basic amino acids, the yields were relatively high (63%--81%). However,when the carboxyl components were N-protected acidic amino acids, the yields were relatively low (47%--48%). The results expanded the application of DEPBT on the synthesis of bioactive peptides containing histidine. 相似文献
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3-(Diethoxyphosphoryloxy)-1,2,3-benzotriazin-4 (3H)-one 1 is a new organophosphorus compound which can be used as an efficient coupling reagent for peptide synthesis by either solution or solid phase coupling. Standard abbreviations for amino acids and protecting groups follow the IUPAC-IUB Joint Commission on Biochemistry Nomenclature: J. Biol. Chem. 1971, 247, 977. 相似文献
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IntroductionEnzymaticpeptidesynthesishasdrawnmuchatten tionbecauseofitsadvantageofenzymestereospecificity ,mildreactionconditions ,minimumside chainprotectionandavoidanceofracemization .Butthestrictsubstratespecificityoftheenzymeslimitstheirapplications .… 相似文献
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Oligosaccharyl Fmoc-asparagine in which amide nitrogen of the asparagine side chain attached to the anomeric position at the reducing end, is a versatile building block and has been used for various glycopeptide synthesis using Fmoc solid-phase peptide synthesis (SPPS). We found unexpected aspartimide formation between amide nitrogen at the reducing end and α-carboxyl acid of oligosaccharyl Fmoc-asparagine during activation of α-carboxyl acid and this side reaction resulted in low coupling yields of oligosaccharyl Fmoc-asparagine with peptide-resin. This aspartimide formed efficiently using conventional coupling reagents such as PyBOP and HATU, but DEPBT afforded little of the aspartimide derivative. Activation condition using DEPBT (3.0 equiv) and DIPEA (2.0 equiv) afforded excellent yield (97%) in coupling reaction between Fmoc-Asn(CHO)-OH and peptide-resin. Based on these results, we performed a synthesis of a sialylglycopeptide, HIV-gp120 (54-63) VVLLVN(CHO)VTENF, in high yield. 相似文献
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Aamal A. Al-Mutairi Fatma E.M. El-Baih Hassan M. Al-Hazimi 《Journal of Saudi Chemical Society》2010,14(3):287-299
Different pyrazolone derivatives were prepared by microwave irradiation and ultrasound assisted methods besides the traditional ones. They were used for synthesis of some derivatives of spiropiperidine-4,4′-pyrano[2,3-c]pyrazole, dihydropyrano[2,3-c]pyrazole, pyrazole-4-carbothioamide, 4-(2-oxo-1,2-diphenylethylidene)-1H-pyrazol-5(4H)-one, azopyrazole, arylmethylenebis-1H-pyrazol-5-ol and araylidene-1H-pyrazol-5(4H)-one via reactions with different reagents applying the ultrasound method in some cases. 相似文献
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Olayinka O. Ajani Craig A. Obafemi Chinwe O. Ikpo Kehinde O. Ogunniran Obinna C. Nwinyi 《Chemistry of Heterocyclic Compounds》2009,45(11):1370-1378
3-Hydrazinoquinoxalin-2(1H)-one was prepared from quinoxaline-2,3-dione and subsequently used for the synthesis of some potentially
biologically active 3-(pyrazol-1-yl)quinoxalin-2(1H)-one derivatives. While 3-(3,5-dimethylpyrazol-1-yl)quinoxalin-2(1H)-one
showed a comparative effect with streptomycin, 3-(5-oxo-3-phenyl-4,5-di- hydropyrazol-1-yl)quinoxalin-2(1H)-one was found
to be the most active with an MIC value of 7.8 μg/ml. 相似文献