采用改进阈值法，测试统计分析了新疆维吾尔自治区内不同地区的7469例（男性3831例、女性3638例）维吾尔族中学生和大学生（12～25岁）苯硫脲尝味能力的阈值分布、味盲率、基因型频率和基因频率。结果显示维吾尔族苯硫脲尝味能力的阈值分布和味盲率具有本民族的自身特点。在新疆维吾尔自治区内，不同地区的维吾尔族苯硫脲尝味味盲率不同，并具有极显著性差异（P＜0?01），从东部（哈密地区）到西部（喀什地区），苯硫脲味盲率逐渐增加，平均味盲率为24?13％，介于欧罗巴人种和其他有色人种之间，该现象与人类学关于现代维吾尔族的族源、人种构成及演化过程的“合流说”相吻合。

With improved threshold method , the genotype frequency and gene frequency of phenylthiourea tasting ability have been tested for 7 469 cases(men 3 831 and women 3 638) Uygur middle school and university students(12~25 years old) w ho live in different areas of Xinjiang Uygur Autonomous Region . The distribution of phenylthiourea tasting ability and phenylthiourea taste blindness rate of Uygur have the nation,s own characteristics .In Xinjiang Uygur Autonomous Region ,Uygur living in different areas have different phenylthiourea taste blindness rate , and have a significant difference ( P<0?01 ) . From the east (Hami area) to the west (Kashi area) , phenylthiourea taste blindness rate gradually increase , average value of taste blindness rate is 24?13% , this value between European and other colored people . This phenomenon coincide with “the theory of confluence” of anthropology on the origin , ethnic composition and evolution of modern Uygur .

本文通过对苯甲酰丙酮与氨基硫脲缩合反应产物的合成和表征，确定了生成物的结构构型。对苯甲酰丙酮与氨基硫脲缩合反应过程中可能存在的加成反应、脱水反应和环合反应，首次采用量子化学计算方法在RB3LYP/6-31G的水平上研究了反应物、产物、中间体复合物和过渡态的优化构型和振动频率，频率分析确定了各中间体稳定性和过渡态的真实性，对每个过渡态均进行内禀反应坐标(IRC)计算以确认它连接着特定的反应物和产物。在RB3LYP/6-311G (2d，2p)的水平上得到了各驻点的能量，分析了苯甲酰丙酮与氨基硫脲的缩合反应途径和机理。机理结果分析表明苯甲酰丙酮与氨基硫脲发生反应时基本分4步进行，氨基硫脲的远端氨基加成到苯甲酰丙酮的远端羰基上生成TM1，TM1进而脱水生成稳定的中间产物PC1，然后PC1发生构象异构化生成TM2，最后氨基硫脲的仲氨氮原子加成到苯甲酰丙酮的近端羰基上形成一个稳定的五元环。

The product compound of the reaction between benzoylacetone and thiosemicarbazide was synthesized and characterized by IR and X-ray diffraction. To the possible addition reaction, dehydration reaction and cyclization reaction in the process of the reaction between benzoylacetone and thiosemicarbazide, the DFT/RB3LYP/6-31G level was firstly adopted to study the optimization configuration and vibration frequency of the reactants and products, intermediates complex and transition state, The data of the frequency of the intermediate and the transition state ensures the stability of the intermediate and the reality of the transition state, intrinsic reaction coordinate (IRC) calculation was run to confirm that each transition state is connected to a specific reactants and products. DFT/RB3LYP/6-311G (2d, 2p) level was also adopted to study the energy of the stagnation points, the way and mechanism of the reaction between benzoylacetone and thiosemicarbazide was studied completely. Results s

对氟苯胺在盐酸的作用下与硫氰酸铵反应得到对氟苯基硫脲,然后在溴的作用下环化得到2-氨基-6-氟苯并噻唑;2-氨基-6-氟苯并噻唑水解并与氯化锌反应得2-氨基-5-氟苯硫酚锌盐;2-氨基-5-氟苯硫酚锌盐与D-丙氨酸-N-羰酐反应得到(R)-1-(6-氟-2-苯噻唑)乙胺。最后,(R)-1-(6-氟-2-苯噻唑)乙胺与L-缬氨酸和氯甲酸异丙酯反应得到目的产物苯噻菌胺,总收率51.2%(以对氟苯胺计)。

P-fluoroaniline reacted with ammonium thiocyanate in the present of hydrochloric acid to give 4-fluoro-phenylthioureas, then 4-fluoro-phenylthioureas reacted with bromine in the solution of chloroform to give the 2-amino-6-fluorol-benzothiazoles. In the present of NaOH, 2-amino-6-fluorol-benzothiazoles hydrolyzed and reacted with ZnCl2 to give the bis(5-fluoro-2-aminothiophenol) zinc salt. (R)-1-(6-fluoro-2-benzothiazoly)ethylamine was prepared by the reaction of bis(5-fluoro-2-aminothiophenol) zinc salt with D-alanine-N-carboxy anhydride. Under the catalytic of NaOH, (R)-1-(6-fluoro-2-benzothiazoly) ethylamine reacted with L-valine and isopropyl chlorocarbonate to give the target production of benthiavalicarb. The total yield is 51.2%(calculation on p-fluoroaniline).

以噻二唑-2-氨甲基酚(1)为原料,与异硫氰酸苯酯反应,以中等到良好的产率得到噻二唑基N-苯基取代硫脲类化合物(3a~3i);而化合物1与活性较高的N,N-二甲胺基硫代甲酰氯反应,则可以得到—NH和—OH同时反应的含有N,N-二甲基硫脲和N,N-二甲基硫代氨基甲酸芳酯官能团的产物.利用核磁共振、红外光谱以及高分辨质谱等手段对产物结构进行了表征.

Thioureas have been widely applied in pesticides and pharmaceuticals because of their unique bio-logical activities, such as insecticidal, anti-inflammatory, anti-allergic, antiviral, antibacterial, etc. And thiodiazole derivatives usually have anti-allergic, alexipharmic and regulation of plant growth biological activi-ty. The compounds containing thiourea and thiodiazole would provide better biological activities simultaneously according biological activity of the superposition principle. A series of thioureas containing thiodiazole was syn-thesized from thiodiazole-2-aminomethyl phenols and phenyl isothiocyanate in moderate to good yields. The reaction condition was warm and the scope of substrates was wide. Furthermore, the thiodiazole-2-aminomethyl phenols reacted with a more active reagent dimethylcarbamothioic chloride to afford novel product with thiourea and carbamothioate groups simultaneously. The reactions could afford good results by stirring for 90 min under 60 ℃ and the

以取代苯酚和氯乙酸为原料,合成取代苯氧乙酸,然后经过酰氯化,酯化得到取代苯氧乙酰基异硫氰酸酯,再和2-氨基-4-苯基噻唑反应得到4种N-(取代苯氧乙酰基)-N''-(4-苯基噻唑-2-基)硫脲类化合物,其中3种化合物为首次报道。化合物结构经1H NMR、IR和元素分析得到确证。初步室内生测结果表明该类化合物具有一定的抑菌活性。

In this paper,Four N-(substituted phenoxyacetyl)-N′-(4-phenyl thiazol-2-yl)thiourea were synthesized by reaction of 2-amino-4-phenylthiazole and substituted phenoxyacetyl isothiocyanates which was prepared by acyl chlorination and esterification of substituted phenoxyacetic acids that were obtained by using chloroacetic acid and substituted phenols as reactant. Three of them were new compounds. Their structures had been determined by 1 H NMR,IR and elemental analysis. The preliminary biological ac-tivities had been tested,and the results showed that most of them exhibited fungus-inhibiting.