Synthesis of 1-(dihydroxypropyl)-5-substituted uracils

Novel 1-(dihydroxypropyl)-5-substituted uracils were synthesized in the reaction of 1-(4-nitrophenyl)-5-substituted uracil derivatives with appropriate aminopropanediols under mild conditions. In the case of 3-amino-1,2-propanediol both racemic and enantiomerically enriched products were obtained. These compounds may be considered as new building blocks for oligonucleotide synthesis.     

5-(2’-羧乙基)-6-烷基-3,4-二氢吡喃酮的合成

吡喃酮是许多天然产物的结构单元,我们曾由4-异丁酰基庚二酸在过量醋酸酐及乙酰氯存在下回流得到7-氧代-8,8-二甲基-△~9-六氢香豆素.本文由二氰乙基-β-二酮进行酮解水解反应得到4-酰基庚二酸1_(a-c)。 在过量醋酸酐、乙酰氯存在下由1_a、1_c为底物进行反应没有得到双环的香豆素衍生物.其产物和单纯以乙酐为缩合剂时的产物2_a、2_c相同,产率分别为68％、63％。2_c可在硫酸铁催化     

High yielding microwave-assisted synthesis of 2-(arylmethyl)amino-4-arylamino-6-alkyl-1,3,5-triazines

An efficient and practical procedure was developed to prepare novel 2-(arylmethyl)amino-4-arylamino-6-alkyl-1,3,5-triazines, starting from dicyandiamide and the corresponding arylamines under microwave irradiation and its scope is demonstrated with a number of examples. The valuable feature of this procedure included the short reaction times, high yields, and easy operation.     

Synthesis of 5-(Arylamino)-1-benzyluracils

The synthesis of novel 5-(phenylamino)-, 5-(benzylamino)-, and 5-(phenethylamino) derivatives of 1-benzyluracil-containing different substituents in the aromatic nucleus has been carried out. Using the Hilbert-Johnson reaction it was found that N₍₁₎-monosubstitution can be achieved via alkylation of trimethylsilyl derivatives of 5-(arylamino)uracils using benzyl bromide. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 887–892, June, 2005.     

1-(6-硝基-2-苯并噻唑)-3-(5-溴-8-喹啉)-三氮烯与Co(Ⅱ)的高灵敏显色反应及其应用

报道了在CPB 存在下,新试剂1-(6-硝基-2-苯并噻唑)-3-(5-溴-8-喹啉)-三氮烯(NBTBQT)与钴的显色反应.在pH 9.5的硼砂-NaOH缓冲介质中,试剂与钴形成2:1 深蓝色络合物,其最大吸收波长位于655 nm处,表观摩尔吸光系数为1.94×105 L·mol-1·cm-1,钴的质量浓度在0～0.24 mg/L 的范围内符合比尔定律.方法应用于维生素B12注射液和水系沉积物的测定.     

Synthesis, Characterization, Spectroscopic Properties of 2-（4-Dimethylaminophenyl）-5-fluoro-6-（morpholin-4-yl）-1H-benzimidazole and its Interaction with Calf Thymus DNA

Benzimidazole compounds have attracted a renewed interest recently owing to theirpotential applications in high-performance composite materials, electronic chemicals,photosensitive materials, and their special potentials in biological and/or medicinalapplication1,2. Typically, aromatic compounds with near planar structures and contain-ing hydrogen-donor groups or groups, which are capable of being protonated, havespecial interactions with DNA via intercalation, hydrogen-bonding, and so on3.Me…     

Multicomponent synthesis and anticancer activity studies of novel 6-(Trifluoromethyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylate derivatives

A series of novel 6-(trifluoromethyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives were obtained in good yields from ethyl 4,4,4-trifluoro-3-oxobutanoate, urea, and aryl aldehyde via Biginelli multicomponent reaction. All the corresponding products 4a–4p were examined against four human cancer cell lines (A549, HepG2, COLO205 and DU145) and compounds 4e, 4i, and 4?m which showed promising anticancer activity have been identified.     

Synthesis of 5-[2-(Phenoxy)ethyl] Derivatives of 6-Methyluracil, 6-Methyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one,and 2-Imino-6-methyl-2,3-dihydro-1H-pyrimidin-4-one

A synthesis of novel derivatives of 6-methyluracil, 6-methyl-2-thioxo-, and 2-imino-6-methyl-2,3-dihydro-1H-pyrimidin-4-one containing a 2-(phenoxy)ethyl substituent at position 5 of the pyrimidine ring has been carried out. It was found that 5-[2-(phenoxy)ethyl] derivatives of 6-methyl-2-thioxo- and 2-imino-6-methyl-2,3-dihydro-1H-pyrimidin-4-one are obtained by the condensation of the corresponding ethyl 3-oxo-2-(2-phenoxyethyl)butanoates with thiourea or guanidine. 6-Methyl-5-[2-(phenoxy)ethyl]uracils can be prepared by treating 6-methyl-5-[2-(phenoxy)ethyl]-2-thioxo-2,3-dihydro-1H-pyrimidin-4-ones with an excess of aqueous monochloroacetic acid solution. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1213–1217, August, 2005.     

The use of aliphatic aldehydes for the synthesis of 4-alkyl-6-amino- 3,5-dicyanopyridine-2(1H)-thiones

The condensation of aliphatic aldehydes with malononitrile and cyanothioacetamide gives 4-alkyl-2,6-diamino-3,5-dicyano-4H-thiopyrans which recyclize into 4-alkyl-6-amino3,5-dicyanopyridine-2(IH)-thiones. The latter are easily S-alkylated with -haloacetonitriles and -haloacetophenones.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 4, pp. 938–942, April, 1996     

Regioselective Deprotection of 1,3-Dibenzyl-5-(N,N-dimethylamino)-6-phenylethyluracil

The deprotection of 1,3-dibenzyl-5-(N,N-dimethylamino)-6-phenyl-ethyluracil I was investigated.A practical,regioselective N3 deprotection of compound I was performed with excellent yield using cyclohexene as a hydrogen donor.     

1,3-二(乙氧基甲基)-5-N,N-二甲氨基-6-甲基尿嘧啶的合成

报道了1,3-二(乙氧基甲基)-5-N,N-二甲氨基-6-甲基尿嘧啶方便、高产率的合成方法. 以6-甲基尿嘧啶(1)为起始物, 经硝化、嘧啶N¹,N ³-烷基化、还原及氨基甲基化, 首次高产率合成了1,3-二(乙氧基甲基)-5- N,N -二甲氨基-6-甲基尿嘧啶(5), 并对其化学结构进行了表征.     

The Colour Reaction of Mercury with 1-(6-Ethoxyl-2-benzothiazolyl)-3-(4-Nitrophenyl)-Triazene and its Application

Thetfiazenereagentswereusedforthedeterminationofcadmium,mercuryandzinc.Wehavesynthesizedthetriazenereagentscontainingheterocyclicring'-'.Recently,annewreagentEtOBTNPTwassynthesized.Becausethereagentcontainsanelectronpropellinggroup(-OCH,CH,)inoneendandanelectronwithdrawinggroup(-NO,)intheotherend,sotheconjugatesystemisenlargedinthemolecularstructure,thisresultinginadvantageofmigrationofelectroniccloud.ThesensitivityofthecolourreactionofEtOBTNPTwithmercuryissuperiortoothertfiazenereage…     

新显色剂1-(4-硝基苯基)-3-(5-氯吡啶)三氮烯的合成及其与镉的显色反应

报道了1-(4-硝基苯基)-3-(5-氯吡啶)三氮烯(NPCPDT)的合成及其与镉的显色反应研究。在Triton X-100的存在下,pH 11.5的Na2B4O7-NaOH缓冲溶液中,该试剂能与镉发生显色反应,镉与NPCPDT形成摩尔比为1∶3的黄色配合物,在440 nm处有一最大吸收,在535 nm处有一最大负吸收。以440 nm为参比波长,535 nm为测量波长进行双波长测定,表观摩尔吸光系数为2.68×105L.mol-1.cm-1,镉的质量浓度在0~0.48μg/mL范围内符合比尔定律。用拟定方法测定废水和环境水样中的微量镉。     

1-(4-硝基苯基)-3-(5-溴-吡啶)-三氮烯的合成及其与镍显色反应的研究

三氮烯试剂是测定镉、汞、锌、镍、铜等金属离子的高灵敏显色试剂[1~3],其中含氮杂环的三氮烯试剂的显色效果更佳[4~6]。为改善试剂的分析性能,提高此类试剂的灵敏度和选择性,合成了未见报道的1-(4-硝基苯基)-3-(5-溴-吡啶)-三氮烯(NPBPDT),并对其与镍的显色反应进行了研究。结     

新的手性源——5-(1-(艹孟)氧基)-2(5-H)-呋喃酮的合成及其不对称 Michael 反应的研究

近年来,手性的丁烯内酯类化合物在合成杂环和天然产物方面起了很重要的作用,我们利用新的手性源,5-(1-氧(艹孟)基)-2(5-H)-     

(2S)-(+)-2-溴-1-(6'-甲氧基-2'-萘基)丙-1-酮的不对称合成

以(2R,3R)-酒石酸二甲酯为手性辅助剂,6-甲氧基-2-丙酰基萘经缩酮化、溴化铜不对称溴化、水解等反应合成了(2S)-2-溴-1-(6'-甲氧基-2'-萘基)丙-1-酮。总收率94%。     

Study on the syntheses of new 1-o-chlorobenzoyl-3-(5''''-substituted phenylamino-6''''-phenyl)-1'''',2'''',4''''-triazinyl ureas

Eight new 1-o-chlorobenzoyl-3-(5'-substituted phenylamino-6'-phenyl)-1',2',4'-triazinyl ureas (5a-h) have been synthesized and their bioactivities were detected.     

1-(5-溴-2吡啶偶氮)-2-萘酚-6-磺酸作指示剂络合滴定连续测定铝和钛

在酸性溶液中加入对铝、钛过量的EDTA标准溶液,在pH4．0煮沸下,铝（Ⅲ）、钛（Ⅳ）与EDTA生成稳定的络合物。以5-Br-PAN-S作指示剂,用硫酸铜标准溶液返滴定过量的EDTA,测定铝钛合量,再用置换法测定钛的量。终点变色敏锐,准确度高,方法用于硅酸盐矿物中铝钛的连续测定,结果满意。     

Synthesis of 3-(3-Alkyl-5-thioxo-1H-4,5-dihydro-1,2,4-triazol-4-yl)aminocarbonylchromones

A series of 3-(3-alkyl-5-thioxo-1H-4,5-dihydro-1,2,4-triazol-4-yl)aminocarbonylchromones has been prepared by oxidation of 3-formylchromone with Jones' reagent followed by reaction with 3-alkyl-4-amino-4,5-dihydro-1,2,4-triazole-5(1H)-thione in the presence of POCl³. The structures of the compounds were confirmed by IR, LC-MS, and ¹H NMR spectra and elemental analyses.