有生物活性的哒嗪酮-氨基甲酸酯类衍生物的合成

氨基甲酸酯衍生物;有生物活性的哒嗪酮-氨基甲酸酯类衍生物的合成     

4-羟基香豆素衍生物的荧光性能

4-羟基香豆素衍生物的荧光性能;水杨酸; 羟基香豆素衍生物; 荧光     

N-烷基壳聚糖衍生物的合成及其对阳离子的吸附性能

烷基衍生物;阳离子吸附性能;N-烷基壳聚糖衍生物的合成及其对阳离子的吸附性能     

N-酰基吡唑衍生物的合成与生物活性

N-酰基吡唑衍生物的合成与生物活性;拟除虫菊酯;1H吡唑衍生物;合成;生物活性     

N1-吡啶甲基-N-芳酰基脲衍生物的合成及生物活性

吡啶衍生物;N1-吡啶甲基-N-芳酰基脲衍生物的合成及生物活性     

二乙炔类脂在气-液界面的单分子膜特性

二乙炔衍生物;衍生物;二乙炔类脂在气-液界面的单分子膜特性     

喹啉电解氢化制备四氢喹啉及其N-乙酰化衍生物的合成

喹啉电解氢化制备四氢喹啉及其N-乙酰化衍生物的合成;电化学还原;N-乙酰衍生物     

有机噻吩类衍生物作为电致变色材料*

噻吩类衍生物包括聚噻吩衍生物和齐聚噻吩衍生物。本文从有目的地设计、合成噻吩类衍生物的角度出发,探索了其作为电致变色材料的应用,综述了噻吩类衍生物作为电致变色材料的最新研究进展。     

两亲性羧甲基壳聚糖衍生物的表面活性研究

将羧甲基壳聚糖与烷基缩水甘油醚在碱性条件下反应,合成了一系列新型的两亲性化合物(2-羟基-3-烷氧基)丙基-羧甲基壳聚糖,对其表面性质的研究结果表明,对同一衍生物,在所研究范围内,取代度越高,降低表面张力的能力及效率越高;对同一取代度的不同衍生物,疏水链越长,降低表面张力的能力越强;对链较短和取代度较大的衍生物,如(2-羟基-3-丁氧基)丙基羧甲基壳聚糖(HBP-CMCHS),在外加电解质存在时溶液的表面张力曲线出现2个转折点,表明可能有分子内胶束形成;而对链较长的衍生物,如(2-羟基-3-十二烷氧基)丙基羧甲基壳聚糖(HDP-CMCHS),则无明显的临界胶束浓度,有外加电解质时表面张力曲线也未出现2个转折点.     

一种芴酮衍生物的合成、晶体结构及其光限幅性能

一种芴酮衍生物的合成、晶体结构及其光限幅性能;芴酮衍生物; 单晶结构; 光限幅性能     

An improved synthesis of a novel α1A partial agonist including a new two-step synthesis of 4-fluoropyrazole

This Letter outlines a new two-step process for the synthesis of 4-fluoropyrazole and its application in an improved synthesis of 4-fluoro-1-[5-fluoro-1-(1H-imidazol-2-yl)-indan-4-ylmethyl]-1H-pyrazole. The original synthesis of 4-fluoro-1-[5-fluoro-1-(1H-imidazol-2-yl)-indan-4-ylmethyl]-1H-pyrazole is also described.     

Synthesis of 5-(trifluoromethyl)cyclohexane-1,3-dione and 3-amino-5-(trifluoromethyl)cyclohex-2-en-1-one: new trifluoromethyl building block

A simple synthesis of 5-(trifluoromethyl)cyclohexane-1,3-dione and 3-amino-5-(trifluoromethyl)cyclohex-2-en-1-one from the sodium salt of methyl or ethyl-4-hydroxy-2-oxo-6-(trifluoromethyl)cyclohex-3-en-1-oate is demonstrated. The compounds represent highly functionalized reactive intermediates for the synthesis of organic and heterocyclic compounds containing a trifluoromethyl group.     

Beta-hydroxy-gamma-lactones as chiral building blocks for the enantioselective synthesis of marine natural products

The enantioselective synthesis of trans-(+)-laurediol, (2S,3S,5R)-5-[(1R)-1-hydroxy-9-decenyl]-2-pentyltetrahydro-3-furanol, and (2S,3S,5S)-5-[(1S)-1-hydroxy-9-decenyl]-2-pentyltetrahydro-3-furanol are described. In addition, a formal synthesis of trans-(-)-kumausyne is also developed. All the synthetic procedures have in common the use of enantiomerically enriched beta-hydroxy-gamma-lactones, easily available by Sharpless asymmetric dihydroxylation (AD) from the suitable beta,gamma-unsaturated ester. The use of Katsuki-Sharpless asymmetric epoxidation (AE) as an additional enantioselective reaction provides cyclic compounds of high enantiomeric purity.     

2'-C-branched ribonucleosides. 2. Synthesis of 2'-C-beta-trifluoromethyl pyrimidine ribonucleosides

[structure: see text]. The first synthesis of 2'-C-beta-trifluoromethyl pyrimidine ribonucleosides is described. 1,2,3,5-Tetra-O-benzoyl-2-C-beta-trifluoromethyl-alpha-D-ribofuranose (3) is prepared from 1,3,5-tri-O-benzoyl-alpha-D-ribofuranose (1) in three steps and converted to 3,5-di-O-benzoyl-2-C-beta-trifluoromethyl-alpha-D-1-ribofuranosyl bromide (5). The 1-bromo derivative (5) is found to be a powerful reaction intermediate for the synthesis of ribonucleosides. The reaction of silylated pyrimidines with (5) in the presence of HgO/HgBr2 affords exclusively the beta-anomers (6-8). Deprotection of (6-8) with ammonia in methanol yields the 2'-C-beta-trifluoromethyl nucleosides (9-11).     

A new family of bis-tetrazole (BIZOL) BINOL-type ligands

The synthesis and characterization of 5-(1-(2-(1H-tetrazole-5-yloxy)naphthalen-1-yl)naphthalen-2-yloxy)-1H-tetrazole (BIZOL) as the first bis-tetrazole BINOL-type ligands is described.     

Facile route to 3,5-disubstituted morpholines: enantioselective synthesis of O-protected trans-3,5-bis(hydroxymethyl)morpholines

[reaction: see text] (3R,5R)-1 R1 & R2 = TBDPS, (3S,5R)-2 R1 = Bn,R2 = TBDPS, (3S,5S)-3 R2 & R2 = Bn. trans-3,5-Bis(benzyl/tert-butyldiphenylsilyloxymethyl)morpholines, promising candidates for the C(2)-symmetric class of chiral reagents, were prepared with excellent optical purity. A key step in the synthesis is the coupling of a serinol derivative with 2,3-O-isopropylideneglycerol triflate or its equivalent. This methodology was extended to the synthesis of chiral trans-3-(benzyloxymethyl)-5-(tert-butyldiphenylsilyloxymethyl)morpholine, a potentially useful chiral building block.     

5-二氰亚甲基-4-二环丙亚甲基-3-[1-(2, 5-二甲基-3-呋喃基)亚乙基]四氢呋喃-2-酮的合成

报道俘精酸酐类化合物(E/Z)4-二环丙亚甲基-3-[1-(2, 5-二甲基-3-呋喃基)亚乙基]四氢呋喃-2, 5-酮的拆分, 及(E)和(Z)-5-二氰亚甲基-4-二环丙亚甲基-3-[1-(2, 5-二甲基-3-呋喃基)亚乙基]四氢呋喃-2-酮 4(E)和4(Z)的合成, 并对它们的光致变色特性进行了初步研究。     

Synthesis of 2′-[2-(5-benzyloxyindolyl)]propylamine derivatives

The synthesis of some 2′-[2-(5-benzyloxyindolyl)]propylamine derivatives 1–15 from 2-(5-benzyloxyindole)carboxyaldehyde ( 16 ) and 2-(5-benzyloxy-1-methylindole) carboxyaldehyde ( 17 ) is reported. Compounds 1–15 have been designed as potential monoamine oxidase A and B inhibitors.     

Process development and large-scale synthesis of NK1 antagonist

A scaleable synthetic route is described to obtain 2-(4-acetylpiperadin-1-yl)-6-[3,5-bis(trifluoromethyl)phenylmethyl]-4-(2-methylphenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one (1, KRP-103) as a neurokinin (NK)(1) antagonist. The key step in the synthesis is the intramolecular cyclization of N-[3,5-bis(trifluoromethyl)phenylmethyl]-N-(3-hydroxypropyl)-4-chloro-6-(2-methylphenyl)-2-methylthiopyrimidine-5-carboxamide (15) which was obtained by amide formation between 4-(2-methylphenyl)-2-methylthio-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid (8) and 3-[3,5-bis(trifluoromethyl)phenylmethylamino]-1-propanol (3). Treatment of 15 with 1,8-diazabicyclo[5,4,0]undec-7-ene provided 6-[3,5-bis(trifluoromethyl)phenylmethyl]-4-(2-methylphenyl)-2-methylthio-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one (6). This intermediate (6) is transformed into the candidate compound (1) by two steps; oxidation, and substitution reaction of the resultant sulfone (7) with 1-acetylpiperazine. This synthetic method is free of chromatographic purification and is amenable to large scale synthesis.     

Liquid crystal polymers containing macroheterocyclic ligands. III. Side chain liquid crystalline polymethacrylates containing mesogenic units based on diarylacetylenes and benzo-15-crown-5

The synthesis and polymerization of 4′-[4-ethynyl-1-(11-methacryloylundecan-1-yloxy) benzene] benzo-15-crown-5 ( 8 ), 4′-[4-ethynyl-4′-(11-methacryloylundecan-1-yloxy) biphenyl] benzo-15-crown-5 ( 15 ), 4′-[2-ethynyl-6-(11-methacryloylundecan-1-yloxy) naphthalene] benzo-15-crown-5 ( 24 ), and 4′-[2-ethynyl-6-(11-methacryloylundecan-1-yloxy)naphthalene]-5′-ethylbenzo-15-crown-5 ( 35 ) is described. The synthesis and characterization of 4′-[4-(4-ethynyl-1-(2-ethynyl-6-(6-hydroxyhexan-1-yloxy)naphthathalene)benzene]) benzo-15-crown-5 ( 29 ) is also presented. Both monomers and polymers were characterized for their mesomorphic behavior. 8 , poly( 8 ), and 15 are crystalline. Due to the insolubility of 15 , poly( 15 ) could not be synthesized. 24 is crystalline, while poly( 24 ) displays a monotropic nematic mesophase. 29 exhibits also a monotropic nematic mesophase. 35 is crystalline, while poly( 35 ) displays an enantiotropic nematic mesophase which is kinetically controlled due to its close proximity to the glass transition temperature.