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Their structures were confirmed by elemental analysis, 1H NMR, and IR spectral data. The preliminary bioassay results showed that α-phenyl-sul-fonylcyclododecanone oxime 2,4-dichlorophenoxy acetate (8p) had inhibition ratio 100% and 80.07% against Digitaria sanguinalis Scop., and 100% and 88.70% against Abutilon theophrasti Medic. at concentrations of 100 and 1 mg/L.

初步生物活性测定结果显示,部分化合物具有一定的除草活性,如α-苯磺酰基环十二酮肟-2,4-二氯苯氧乙酸酯(8p)在浓度为100和1 mg/L时对马唐的抑制率分别为100%和80.07%;对苘麻的抑制率分别为100%和88.70%。

It involved the converstion of vanillin into hydrazine (4) and the metalic reduction of hydrazine 4 into the intermediate vanillic amine.

以价廉易得的香草醛为起始原料,经过3步反应,高产率合成了酚羟基由对甲苯磺酰基保护的香草胺类化合物5。

They are, 4 21-amidohydrocortisone Ba1~Ba4, 10 21-amidoprednisolone Bb1~Bb10, 4 21-amidomethylprednisolone Bc1~Bc4, 4 21-amidodexamethasone Bd1~Bd4, 1 21-amidobetamethasone Be1, 1 21-amidoRS Bf1, 1 21-amidocortisone Bg1, 1 21-amidoprednisone Bh1. The amido groups were acetamido, nicotinamido, hemesuccinamido, benzoylamido, methanesufonamido, or arylsufonylamido.

包括:4个21-酰胺基氢化可的松(Ba1~Ba4),10个21-酰胺基氢化泼尼松(Bb1~Bb10),4个21-酰胺基甲泼尼龙(Bc1~Bc4),4个21-酰胺基地塞米松(Bd1~Bd4),1个21-酰胺基倍它美松(Be1),1个21-酰胺基RS(Bf1),1个21-酰胺基可的松(Bg1),1个21-酰胺基强的松(Bh1)。21-酰胺基分别为乙酰胺基、烟酰胺基、单琥珀酰胺基、苯甲酰胺基、甲烷磺酰胺基或取代苯磺酰胺基等。

A series of p-toluene sulfonylamido acetacylhydrazone derivatives were synthesized from p-toluenesulfonyl chloride which reacted with glycine to get the intermediate p-toluene sulfonylamido glycine, then through the esterification, hydrazinolysis to afford another intermediate p-toluene sulfonylamido acethydrazide, which condensed with different aldehydes to obtain the target compounds that were characterized by IR, 1H NMR, 13C NMR spectra and elemental analysis.

魏太保 ;冷艳丽;王永成;张建辉;张有明*摘要:以对甲苯磺酰氯为原料,通过与氨基乙酸反应得到中间体对甲苯磺酰氨基乙酸,再经酯化、肼解得到对甲苯磺酰氨基乙酰肼,然后与相应的醛缩合得一系列对甲苯磺酰胺基乙酰腙类化合物。其结构经元素分析, IR, 1H NMR和13C NMR确证。

In part one, the reactions of some active fluorine-containing compounds such as 2, 2-dihydropolyfluoroalkanoic acids and ethyl 2-hydropolyfluoroalkenoates were studied and various fluorine-containing heterocyclic compounds were synthesized. Using 2, 2-dihydropolyfluoroalkanoic acids as the starting material, 4-fluoroalkyl quinolin-2-ols, 2- [ -1-hydropolyfluoro-1-alkenyl] -4H-3, 1-benzoxazin-4-ones, 1-aryl -4, 9-dihydro-3-fluoro-alkyl-1H-pyrazo [3, 4-b] quinolin-4-ones, 5-fluoroalkyl-12H-quin olino [2, 1-b] quinazolin-12-ones, 4-fluoroalkyl-1, 3-dihydro-1, 5-benzodiazepin-2-ones and 4-fluoroalkyl-2H-pyrido [1, 2-a] pyrimidin-2-ones were synthesized through its condensation reaction with anilines, anthranilic acid, N'-aryl-o-aminobenzamides, o-nitro aniline, o-amino pyridine and their derivatives and the subsequent transformations. 5-Fluoroalkyl isoxazolidines, 3-fluoro-3-fluoroalkylisoxazolidino [4, 3-c] quinolin-4-ones, 3-fluoroalkylisoxazolino [4, 3-c] quinolin-4-ones and 2-aryl-3per fluoroacylindoles were synthesized by inter-and intramolecular 1, 3-dipolar cycloaddition of fluorine-containing olefins and nitrones.

第二部分,我们研究了α,α-二氟苄基卤类化合物的亚磺化脱卤反应、产物的转化及全氟烷基亚磺酸盐与芳环化合物的全氟烷基化反应,发现全氟苄基碘或溴及α,α一二氟苄基溴在保险粉等亚磺化脱卤试剂引发下可生成相应的亚磺酸盐;全氟苄基亚磺酸盐与氯气或溴反应可生成全氟苄基磺酰氯或磺酰溴;在烯烃存在下,全氟苄基碘则与烯烃发生加成反应,生成相应的1:1加成产物;在三价醋酸锰的作用下,部分芳香化合物如茴香醚,二甲氧基苯,吡啶,喹啉等可以和过量的全氟烷基亚磺酸盐发生双全氟烷基化反应,反应表现出一定的区域选择性,产率良好。

Synthesis of α-(p-Toluenesulfonamido)-Phosphonic Acid Derivatives and Phosphonopeptides and Their Biologic Activity PH.D.

为寻找高效选择性除草剂,我们设计、合成了新型含磺酰基α-氨基膦酸和膦肽衍生物共96个,并研究了有关的化学反应。

The alkylation of a-methylene of PhSO2CH2COPh with alkyl halides catalyzed by quaternary ammonium base resin in 50% aqueous sodium hydroxide solution was investigated.

本文以季铵碱树脂作为聚合物固载的相转移催化剂,在50%氢氧化钠水溶液中催化α-苯磺酰基苯乙酮(1)的α-亚甲基的烷基化反应。

During the research, one of the best stereoselective results was achieved in Streckerreactions on the aliphatic imines and the possible mechanism was proposed.

在研究过程中,我们发现在CsF促进下TMSCN能够对有α-氢的亚磺酰基亚胺进行高非对映选择性的加成反应并取得迄今为止脂肪族亚胺的Strecker反应的最好结果。

The results ofthe addition of lithium phosphine showed the operation of a double stereo-differentiation effect and the chirality of the sulfinyl group dominated the asymmetricinduction.

在亚磷酸锂盐的加成反应中,这两个手性基团起双重诱导作用,其中亚磺酰基的手性中心起主导作用。

The Research about the Synthesis of Phenylsulfonyl α,β-unsaturated Ketones and Their Applications in Asymmetric Diels-Alder Reaction Catalyzed by Lewis Acid and Chiral Titanium Reagents.

磺酰基取代的α,β-不饱和酮的合成及其在不对称催化Diels-Alder反应中的研究

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