Metabolism of N-phenyl-2-naphthylamine andN-phenyl-1-naphthylamine by rat hepaticmicrosomes and hepatocytes

The carcinogenic antioxidants,N-phenyl-1-naphthylamine (P1NA)and N-phenyl-2-naphthylamine (P2NA) were examined in vitro for biotransformation by rat hepatic microsomes and in freshly isolated hepatocytes. HPLC-analysis of hepatocyte incubations with revealed that phenols were the major metabolites in both cases. P1NA formed one phenolic metabolite only, while incubation with P2NA yielded two phenols identified as 6-hydroxy-P2NA and 4'-hydroxy-P2NA by cochromatography with authentic samples. β-naphthylamine, a metabolite indicating dephenylation of P2NA was not detectable.Metabolism studies with microsomes revealed that the phenols were formed by cytochrome P-450 dependent monooxygenases. Pretreatment of animals with phenobarbital and 3-methylcholanthrene both increased the rate of microsomal metabolism of P1NA and P2NA, indicating that more than one P-450 enzyme mediate the oxygenation reaction. Animal pretreatment with single and repeated doses of P1NA and P2NA did not markedly stimulate metabolism, but induced ethylmorphine demethylatior. in males and females and benzo (a)pyrene hydroxylation in females.

Structure Study on N-Phenyl-2-deoxy-D-ribopyranosylamine

The title compound N-phenyl-2-deoxy-D-ribopyranosylamine featuring a single conformation and pyranose-ring has been synthesized and characterized by NMR spectrum and X-ray diffraction. X-ray crystal structure analysis shows that its crystal belongs to the monoclinic system, space group P21 with a = 6.5375（9）, b = 7.7140（9）, c = 10.7865（16）A, β= 97.578（11）^o, Z = 2, V= 539.22（13）A^3, Dc = 1.289 g/cm^3, F（000） = 224, μ（MoKa） --- 4.533 mm^-1, R = 0.0305 and wR = 0.0639 for 1093 observed reflections （I 〉 2σ（I）. This compound exists as a-conformation and ^1C4 chair-like configuration.

Synthesis and Herbicidal Activity of Novel N-（2-Fluoro-5（3- methyl-2,6-dioxo-4-（trifluoromethyl）-2,3-dihydro-pyrimidin- l（6H）-yl）phenyl）-2-phenoxyacetamide Derivatives

Thirteen novel N-（2-fluoro-5-（3-methyl-2,6-dioxo-4-（trifluoromethy）-2,3-dihydropyrimidin-1（6H）-yl）phenyl）- 2-phenoxy）acetamides were designed and synthesized utilizing 4-fluoro-aniline and ethyl 3-amino-4,4,4-trifluoro-but-2-enoate as starting materials. The chemical structures of all compounds were confirmed by IH NMR, IR, mass spectrum and elemental analyses. Subsequently, the herbicidal activities of the as-prepared compounds were evalu-ated in the greenhouse. Bioassay results indicated that most of compounds had better herbicidal activities against dicotyledonous weeds. Among all the tested compounds, compounds 4a--4i showed good herbicidal activities at both pre-emergence and post-emergence treatment against two or three kinds of dicotyledonous weeds, such as Abutilon theophrasti Medic, Amaranthus ascendens L, and Chenopodium album L at the dosage of 75 g ai/ha.

新显色剂PMNHA的合成、分析鉴定及其在分光光度测定钒中的应用

用１－甲基－２－萘甲酰基替换Ｎ－苯甲酰苯基羟胺（ＢＰＨＡ）的苯甲酰基，合成了一种新显色剂Ｎ－苯基－１－甲氧基－２－萘甲酰氧肟酸（Ｎ－ｐｈｅｎｙｌ－１－ｍｅｔｈｏｘｙ－２－ｎａｐｈｔｈｏｙｌｈｙｄｒｏｘａｍｉｃａｃｉｄ，缩写为ＰＭＮＨＡ）。根据元素分析、差热分析、质谱分析、核磁共振、红外光谱分析，确定ＰＭＮＨＡ的组成和结构为：ＯＣＨ３ＣＯＮＯＨＣ６Ｈ５。该试剂的三氯甲烷溶液能很快从２．２５—４．５０ｍｏｌ／ＬＨＣｌ中萃取钒（Ⅴ）的紫色配合物，其配合物最大吸收在５４０ｎｍ，很多外来离子，特别是大量的钛不干扰钒的测定，钒含量在０—２８μｇ·ｇ－１范围遵守比耳定律。

Copper(Ⅱ)-Catalyzed Synthesis of N-Substituted-3-amino-4- cyano-isoquinoline-1(2H)-ones by the Reaction of N-Substituted-2-iodobenzamides with Malononitrile

A novel Cu(OAc)_(2)•H_(2)O catalyzed coupling reaction of N-substituted-2-iodobenzamides with malononitrile to afford N-substituted-3-amino-4-cyano-isoquinoline-1(2H)-ones is described.The reaction proceeded in DMSO at 90℃ for 5 h in nitrogen without external ligands.