An Efficient Synthesis of 2-CF3-3-Benzylindoles

The reaction of α-CF₃-β-(2-nitroaryl) enamines with benzaldehydes afforded effectively α,β-diaryl-CF₃-enones having nitro group. Subsequent reduction of nitro group by NH₄HCO₂-Pd/C system initiated intramolecular cyclization to give 2-CF₃-3-benzylindoles. Target products can be prepared in up to quantitative yields. Broad synthetic scope of the reaction was shown. Probable mechanism of indole formation is proposed.     

An Inexpensive,Efficient Synthesis of 1-Methylxanthine

1-Methylxanthine has been prepared in 20% overall yield via a reproducible six-step sequence.     

A New and Efficient Synthesis of 2H-3, 1-Benzoxazine Compounds

2H-3, 1-Benzoxazine heterocyclic compounds are a series of potent nonsteroidal pro- gesterone receptor agonists1-3 and have many other applications such as carbonaceous electrode, plant growth regulating and anti-stress activities4-6, etc.. Comparing to other benzoxazine series, such as 1, 4-benzoxazine, 2H-1, 3-benzoxazine, etc., little attentions have been paid for this series of compounds. There is only one method for the preparation of 2H-3, 1-benzoxazine, e.g. cyclocondensation of o-amin…     

An Efficient Synthesis of 3-Cyano-1(3H)-Isobehzofuranones

Reaction of o-formyl-N, N-diethylbenzamides (5) with trimethylsilyl cyanide affords the corresponding (0-trimethylsi-lyl)cyanohydrins (6), which on treatment with acetic acid produce 3-cyanophthalides (7) in 80–90% isolated yields.     

An Efficient Synthesis of 1-Triacontanol

The recent efficacy of 1-triacontanol (1) as a plant growth stimulant¹, coupled with the fact that the responses of both rice and tomatoes to a synthetic sample are similar to that of natural triacontanol: has directed attention towards its svnthesis^2,3. As this compound 1 has the potential for commercial use, emphasis has been placed on simple procedures which are amenable to large scale preparation.     

短肽5－氟尿嘧啶前体药物的合成及其抗肿瘤活性研究

短肽５－氟尿嘧啶前体药物的合成及其抗肿瘤活性研究罗毅,卓仁禧,范昌烈（武汉大学化学系,武汉,４３００７２）关键词氨基酸,短肽,５－氟尿嘧啶,抗肿瘤活性５－氟尿嘧啶（５－ＦＵ）是一种治疗癌症的广谱性抗代谢药物,但由于其毒副作用较大,从而限制了它在临床上...     

An Efficient Synthesis of 2-Cyclohexene-1-Carboxylic Acid and 2-Cyclopentene-1-Carboxylic Acid

A simple and efficient synthesis of the title compounds by modified Grignard methodology is described.     

Synthesis of (2R, 3S, 4R)-2-Hydroxymethyl-3,4-Dihydroxypyrrolidine Hydrochloride from D-Glucose

(2R, 3S, 4R)-2-Hydroxymethyl-3,4-dihydroxypyrrolidine hydrochlo-ride was synthesized from diacetone-D-glucose.     

2-Hydroxymethyl-2-propyl-1,3-propanediol in the Synthesis of Phospholipids

New representatives of nonglycerol polyol phospholipids were synthesized from 2-hydroxymethyl-2-propyl-1,3-propanediol through intermediate phosphoramidites and cyclic phosphites obtained from isopropylidene derivative of the title triol. Treatment of these intermediate products with sulfur or selenium afforded the corresponding thio- and selenophosphates which were converted into lipids by direct acylation with higher carboxylic acid chlorides.__________Translated from Zhurnal Organicheskoi Khimii, Vol. 41, No. 7, 2005, pp. 983–987.Original Russian Text Copyright © 2005 by Savin, Kamneva.     

Mild and Efficient Tf2O-Mediated Synthesis of 3-Amino-1-benzofurans

Russian Journal of Organic Chemistry - A mild and efficient procedure has been developed for the synthesis of 3-amino-1-benzofurans by intramolecular cyclization of the corresponding...     

An Efficient One-Pot Synthesis of 3-(2-Benzothiazolyl)coumarins

Some 3-(2-benzothiazolyl)coumarin imines and 3-(2-benzothiazolyl)coumarins are prepared from 2-benzothiazolylacetonitrile and 2-hydroxybenzaldehydes in ethanol in the presence of catalytic amount of NaOH.     

An Efficient Synthesis of Benzopyrano-2-Isoxazolines

A series of benzopyrano-2-isoxazoline compounds have been prepared efficiently by three-step synthesis from corresponding salicylaldehyde derivatives.     

Oxidation Reactions of Azines. 10. Synthesis, Structure, and Oxodihydroxylation of 3-Hydroxymethyl-1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine

It has been established that oxidation of a mixture of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine and dicyanomethane or formaldehyde with manganese dioxide gives 3-hydroxymethyl-1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, the structure of which was confirmed by X-ray structural analysis. Some oxidative conversions by potassium permanganate of the product formed and its esters have been studied. These included lactamization, aromatization, and oxodihydroxylation.     

An Efficient Synthesis of 4,5-Dihydro-3(2H)-pyridazinone Derivatives

Reaction of hydrazine with 5-(2-aryl-2-oxo-ethan-1-yl)-5-R Meldrum's acids 3 gives 4,6-disubstituted 4,5-dihydropyridazin-3(2H)-ones 4 at room temperature. The method is simple and the yield is good. The production of the starting material 3 also is discussed.     

An Efficient Solid-State Synthesis of N-Aryl-2-phenyldiazenecarboxamides

The subject of organic solid-state synthesis is a fascinating one. It has many advantages such as high efficiency and selectivity, easy separation and purification, mild reaction conditions, and environmental acceptability1. In recent years, this method has been widely used in a variety of organic reactions including substitution2, condensation3, oxidation-reduction4, rearrangement5 and elimination6. However, the solid state reaction using K3Fe(CN)6/KOH to oxidize substituted semicarbazides…     

An Efficient Synthesis of 4-Phenyl-2-aminoquinolines

An efficient procedure for 3-substituted-4-Phenyl-2-aminoquinolines involving the reaction between a preformed complex of amide 2 and phosphorus oxychloride with o-acetamidobenzophe one is reported. Hitherto unknown ten 4-Phenyl-2-aminoquinolines have been synthesized in 72–88% yield.     

An Efficient One-Pot Synthesis of 2-Hydroxyalkyl Dithiocarbamates

Abstract

In the presence of anhydrous potassium phosphate, epoxides reacted with carbon disulfide and primary or secondary amines in acetone to give the corresponding 2-hydroxyalkyl dithiocarbamates regioselectively in moderate to good yield.     

Synthesis of Phospholipids on the Basis of 2-Hydroxymethyl-2-propyl-1,3-propanediol

Russian Journal of Organic Chemistry -     

An Efficient Synthesis of (±)-α-Spirovetivene and Related Compounds

A process for the synthesis of (±)-α-spirovetivene starting from I-oxo–2-carbethoxy-6, 10-dimethyl spiro[4.5]dec-6-ene(I)¹ is described. The oxo group of I was reduced by the process of Coates², and the resulting spiro ester (III) and spiro alcohol (IV) were transformed to (±)-α-spirovetivene by the process of Uijttewaal³ and by conventional methods.