Hydrogen bonding and sodium coordination in the crystal structure of tetrasodium (3-((2,4-dinitrophenyl)amino)-1-hydroxypropane-1,1-diyl)-bis-phosphonate pentahydrate – a N-substituted Pamidronate

The reaction of 1-fluoro-2,4-dinitrobenzene with (3-amino-1-hydroxypropane-1,1-diyl)bis(phosphonic acid) (pamidronic acid) 1a in combination with NAOH leads to disodium (3-((2,4-dinitrophenyl)amino)-1-hydroxy-propane-1,1-diyl)bis(phosphonate) heptahydrate 2 and further to tetrasodium (3-((2,4-dinitrophenyl)amino)-1-hydroxy-propane-1,1-diyl)bis(phosphonate) pentahydrate 3. The crystal structure of 3 is composed of the organic anion, which is coordinated to the sodium counter cations and furthermore is involved in hydrogen bonds. The 2,4-dinitrophenyl moiety gives rise to π–π connected hydrophobic layers. The hydrophilic moiety of the anions, sodium cations and water molecules form a hydrophilic layer. The individual conformation of this N-substituted pamidronate anion is a compromise between its geometric limitations and the intermolecular interactions with sodium and the water molecules.     

Synthesis and Cyclization of N-(4-Phenoxyphenyl)-β-alanines

We have used the reaction of 4-aminodiphenyl ester with acrylic, methacrylic, crotonic, and itaconic acids to synthesize N-substituted -alanines, which undergo ring closure to form derivatives of dihydropyrimidinedione and 4-carboxy-2-pyrrolidinone. We have studied the reactions of acylation and recyclization of the dihydropyrimidinedione ring, and we have synthesized derivatives of 4-carboxy-1-(4-phenoxyphenyl)-2-pyrrolidinone: arylidene hydrazides, 2[(2-oxo-4-pyrrolidinyl-1-(4-phenoxyphenyl)]benzimidazole.     

Synthesis of Pyrazole Derivatives Possessing Anticancer Activity: Current Status

Pyrazole is a versatile lead compound to design potent bioactive molecules for drug discovery and development, particularly in cancer therapy. The aim of this review is to present the most recent deeds in the field of synthetic route made for functionalized pyrazole derivatives active against cell proliferation disease. The review article covers the synthesis of 1H-pyrazole, synthesis of N-substituted pyrazoles, synthesis of pyrazolopyrazoles, and synthesis of pyrazoles fused with a naturally occurring moiety. Some of these reported compounds have passed the preclinical or initial-phase clinical trials for their anticancer activity.     

Six cation-templated halometal complexes and C–H activation of alkylene-bridged azoles

Six dication-templated complexes were discovered in efforts to investigate the effect of linear imidazolium-based template, 1,ω-bis(3,3′-methylimidazolium)alkyl dibromide, on pure inorganic halometal clusters. Complexes {[C₄(Mim)₂](Pb₂I₆)}_n (1) (ω?=?4), {[C₁(Mim)₂] (Ag₂I₄)}_n (2) (ω?=?1), {[C₃(Mim)₂](Ag₂I₄)}_n (3) (ω?=?3), and {[C₄(Mim)₂](Ag₂I₄)}_n (4) (ω?=?4) possess 1-D chain architecture with different organic cations trapped in it. Compound {[C₃′(Mim)₂](CuBr₃)} (5) (ω?=?3) contains the mononuclear anion (CuBr₃)^2? and intra-molecular coupled organic cation with the formed seven-membered ring. {[C₂(Mim)₂S₂]₂(Cu₂I₂)}_n (6) (ω?=?2) presents an infinite 2-D coordination polymer as the first representative polyrotaxane example featuring the biimidazolium thiolate cation ligand. All compounds were further characterized with IR spectra and thermal analysis properties.     

含吡啶环的1,3,4-噁二唑衍生物的合成及生物活性研究

依据生物电子等排原理,在分子中同时引入吡啶环和1,3,4-噁二唑杂环合成了5-(3-吡啶基或4-吡啶基)-1,3,4-噁二唑2-硫乙酸胺类化合物,用¹HNMR,IR,质谱和元素分析对其结构进行了表征.离体试验表明,化合物B1-5小麦赤霉病菌和苹果轮纹病菌的抑制率分别为30%和42%,化合物B1-6对苹果轮纹病菌的抑制率为38%.除草活性实验结果表明,化合物B1-6对油菜和稗草具有较高的抑制作用.     

N-芳基(烷基)-N′-芳基(烷基)-N″-(葡萄糖基硫代亚脲基)膦酰三胺的合成

膦酰三胺类化合物具有优良的杀菌、抗病毒作用,其中部分还有抗肿瘤活性。脲和硫脲类化合物及其衍生物既具有优良的杀菌、除草等活性,又是一种重要的有机合成中间体。它的糖基衍生物是生物体内重要的代谢产物,具有维持代谢水平,提高机体耐受力等生理活性。糖基的多羟基特点,有利于增加这些化合物的水溶性,