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The relative stabilities of 6-membered cyclic allylamine/enamine systems

Evidence on the relative stabilities of acyclic allylamine/enamine systems and methods for the isomerisation of the former into the latter are reviewed. Previous evidence on the related question of the thermodynamic stabilities of 3-piperideines/2-piperideines is presented. The view that 6-membered cyclic allylamines are thermodynamically preferred over their enamine isomers is refuted by demonstrating the base-catalysed equilibrative isomerisations of several 1-alkyl-4-acyl-1,2,5,6-tetrahydropyridines into their 1-alkyl-4-acyl-1,4,5,6-tetrahydropyridine isomers. It is shown that the conjugated CO group in these examples is unnecessary to effect isomerisation: for example even in the simplest possible situation, 1-methyl-1,2,5,6-tetrahydropyridine can be isomerised into 1-methyl-1,4,5,6-tetrahydropyridine, though a stronger base is necessary.     

The conversion of a pyrrole trimer derivative into a 4,5,6,7‐tetra­hydro‐4‐­(pyrrol‐2‐yl)indol‐7‐yl­tosyl­aminoindole

Vilsmeier formyl­ation of trans‐1‐(4‐methyl­phenyl­sulfonyl)‐2,5‐bis(pyrrol‐2‐yl)­pyrrolidine leads to cleavage of the central ring then a reclosure resulting in the formation of trans‐N‐[2‐formyl‐4‐(5‐formyl­pyrrol‐2‐yl)‐4,5,6,7‐tetra­hydro­indol‐7‐yl]­toluene­sulfon­amide, C₂₁H₂₁N₃O₄S.     

Spiro[4H‐pyran‐3,3′‐oxindoles] Derived from 1,2,3,4‐Tetrahydroquinoline

Three‐component reactions of 5,6‐dihydro‐4H‐pyrrolo[3,2,1‐ij]quinoline‐1,2‐dione with malononitrile, or ethyl cyanoacetate, and cyclic six‐membered or a five‐membered 1,3‐diketone, produce spiro[4H‐pyran‐3,3′‐oxindoles].     

The Synthesis of 6‐Substituted Pyrido[2,3‐d]pyrimidine‐2,4(1H,3H)‐diones Using Aminomethylene Malondialdehydes and 6‐Aminouracils

Variously substituted aminomethylene malondialdehydes (2‐(3,3‐dimethylindolin‐2‐ylidene)malondialdehydes) were reacted with some 6‐aminouracils, to give 6‐(3,3‐dimethyl‐3H‐indol‐2‐yl)pyrido[2,3‐d]pyrimidine‐2,4‐(1H,3H)‐diones in good yields.     

抗坏血酸有机锗倍半氧化物的合成及抗癌活性研究

通过三氯锗仿与抗坏血酸分子的加成反应,合成了一种新型有机锗倍半氧化物,产物的结构通过元素分析、IR及UV光谱等方法进行了表征．生物活性实验表明合成物对小鼠S-180肿瘤生长具有显著的抑制作用．