中国科技论文在线

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2008年04月08日

【期刊论文】Synthesis and biological evaluation of novel naphthoquinone fused cyclic aminoalkylphosphonates and aminoalkylphosphonic monoester

苗志伟， B. Wang，， Z. W. Miao， J. Wang， R. Y. Chen， X. D. Zhang

Amino Acids (2007)，-0001，（）：

-1年11月30日

摘要

A series of novel naphthoquinone fused cyclic α-aminophosphonates, 2-alkoxy-3, 4-dihydro-2H-naphtho[2,3-e][1,4,2] oxazaphosphinane-5, 10-dione 2-oxide 3–17 and naphthoquinone fused cyclic α-aminophosphonic monoester 18 were synthesized for the first time. These cyclic α-aminophosphonates were evaluated for antitumor activity on four human tumor cell lines, and three of them showed significant cytotoxicity (IC50: 0.019–5.15 μM) comparable to that of the reference drug doxorubicin. Furthermore, inhibition assays for topoisomerase II-mediated relaxation of supercoiled DNA indicated that the naphthoquinone fused cyclic aminophosphonates were catalytic inhibitors of topoisomerase II.

Amino acid， Aminoalkylphosphonic acid， Topoisomerase II inhibitors， Mannich-type reaction， Phosphorus heterocycles

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2008年04月08日

【期刊论文】 aldehydes (ketones) under solvent-free and catalyst-free conditions—synthesis of N-phosphoramino α-aminophosphonates

苗志伟， Jianfeng Zhang， Zhanwei Cui， Fei Wang， Yadan Wang， Zhiwei Miao， Ruyu Chen

Green Chem., 2007, 9, 1341–1345，-0001，（）：

-1年11月30日

摘要

A convenient and rapid method was developed for the synthesis of various N-phosphoramino α-aminoalkylphosphonates through Mannich type reactions under catalyst- and solvent-free conditions with excellent yields.

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2008年04月08日

【期刊论文】Synthesis of Diphenyl α-(Dipropoxyphosphoramido) alkyl-phosphonates

苗志伟， CUI Zhan-Wei， ZHANG Jian-Feng， MIAO Zhi-Wei， CHEN Ru-Yu

Chinese Journal of Chemistry, 2007, 25, 1551—1554，-0001，（）：

-1年11月30日

摘要

A convenient method has been developed for the synthesis of diphenyl α-(dipropoxyphosphoramido) alkyl- phosphonates under mild conditions, namely the reaction of dipropyl phosphoramidate (1) with a para-(un)substituted benzaldehyde or cyclicketone (2) and triphenyl phosphite (3) by a one-pot procedure with the aid of acetyl chloride.

Mannich type reaction， α-aminoalkanephosphonate， triphenyl phosphate， acetyl chloride

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2008年04月08日

【期刊论文】Full Paper Synthesis and Electrospray Ionization Mass Spectra of N-(1, 3, 2-Dioxaphosphorinan-2-ylmethyl) thiophosphoramidates

苗志伟， MIAO Zhi-Wei， FU Cui-Rong， WANG， Bin， CUI Zhan-Wei， ZHANG Jian-Feng， CHEN Ru-Yu

Chinese Journal of Chemistry, 2007, 25, 1344—1348，-0001，（）：

-1年11月30日

摘要

N-(1,3,2-Dioxaphosphorinan-2-ylmethyl) thiophosphoramidates were synthesized and determined by NMR spectra and positive ion electrospray ionization mass spectrometry (ESI-MS) in conjunction with tandem mass spectrometry (MS/MS). The fragmentation pathways were investigated. The results show that these characteristic ions in ESI mass spectra are useful in the structural determination of N-(1, 3, 2-dioxaphosphorinan-2-ylmethyl)- thiophosphoramidates.

ESI-MS， N-(， 1,， 3,， 2-dioxaphosphorinan-2-ylmethyl)， thiophosphoramidate， conjugate， tandem mass spectrometry

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2008年04月08日

【期刊论文】A Simple and Convenient Procedure for the Synthesis of Naphthoquinone Fused Cyclic α-Aminophosphoryl Chloride

苗志伟， Bin Wang， Zhiwei Miao， Ruyu Chen

Heteroatom Chemistry Volume 18, Number 4, 2007，-0001，（）：

-1年11月30日

摘要

The synthesis of a novel quinone fused phosphorus heterocycle, 2-chloro-3, 3-disub- stituents-3, 4-dihydro-2H-naphtho[2, 3-e][1, 4, 2]-oxazaphosphinane-5, 10-dione 2-oxide (3a–g), was described for the first time. These compounds, which have a readily leaving group Cl, can serve as intermediates of many quinone fused phosphorus heterocycles. The structures of 3a–g were characterized by using common spectroscopic methods. According to the X-ray structure of 3a, these compounds may be used as DNΑ-intercalators.

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