具有抗癌活性的新型4-苄基-1(2H)-酞嗪酮衍生物的便捷合成

S. E. Rayes, I. Ali, hamdy Abd Elazeem, Sara Eltorky
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摘要

合成了一系列新的具有生物活性的酞嗪酮衍生物。从4-苄基-1(2 H)-酞嗪酮1的乙酰肼通过叠氮偶联法合成的4-苄基-1(2 H)-酞嗪酮2a的氨基酸甲酯入手。以相应的酯类2a、b为原料,通过肼水解制得3a、b。通过叠氮偶联法,相应的肼3a分别与胺和氨基酸酯反应得到N -取代-2-(4-苄基-1-氧- 1h -酞嗪-2-基)-甲基-乙酰胺4a-f和二肽甲基{2-[2-(4-苄基-1-氧- 1h -酞嗪-2-基)-乙酰氨基]-乙酰氨基}-烷酸酯6a-c。类似的;通过叠氮偶联法,将相应的肼3b分别与胺类和氨基酸酯类反应,得到N -取代- 3-[2-(4-苄基-1-氧- 1h -酞嗪-2-基)-乙酰氨基]-丙酰氨基烷酸酯7a-c和二肽甲基{3-[2-(4-苄基-1-氧- 1h -酞嗪-2-基)-乙酰氨基]-丙酰氨基烷酸酯7a-c
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Convenient Synthesis of Some Novel 4-Benzyl-1(2H)-Phthalazinone Derivatives of expected anticancer activity
Series of new synthesized biologically active phthalazinone derivatives were obtained. Starting from the amino acid methyl esters of 4-benzyl-1(2 H )-phthalazinone 2a,b which were synthesized from the aceto hydrazide of 4-benzyl-1(2 H )-phthalazinone 1 via azide coupling method. The hydrazides 3a,b were prepared from hydrazinolysis of corresponding esters 2a,b . N -substituted-2-(4-Benzyl-1-oxo-1H-phthalazin-2-yl)-methyl-acetamide 4a-f and the dipeptides methyl {2-[2-(4-Benzyl-1-oxo-1H-phthalazin-2-yl)-acetylamino]-acetylamino}-alkanoates 6a-c were obtained by the reaction of corresponding hydrazide 3a with amines and amino acid esters respectively via azide coupling method. Similarly; N - substituted - 3 -[2-(4-Benzyl-1-oxo-1H-phthalazin-2-yl)-acetyl amino] propionamide 5a-f and the dipeptides methyl{3-[2-(4-Benzyl-1-oxo-1H-phthalazin-2-yl)-acetylamino]-propionylamino} alkanoates 7a-c were obtained by the reaction of corresponding hydrazide 3b with amines and amino acid esters respectively via azide coupling method
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