Current Organic Synthesis - Volume 12, Issue 2, 2015

The importance of diaminomaleonitrile (DAMN) as a readily available and cheap building block for the synthesis of various nitrogen heterocycles has attracted the attention of organic chemists worldwide. An enormous number of research studies have focused on the preparation of various heterocycles that play a role in the pharmaceutical, cosmetics, dyes, and pigment industries, among others. This review details develop Read More

Saccharide microarray technology has emerged as a powerful tool for studying the interactions of saccharides with a variety of biomolecules in high-throughput manner. An efficient and selective immobilization technique of saccharides on the surface is essential for successful preparation of saccharide microarrays. Carbohydrates can be immobilized on the support surface by covalent or noncovalent binding. The methods of Read More

Organoselenium compounds have attracted special attention over the last years mainly because of their diversified biological activity. In particular, 1,3-selenazoles are interesting five-membered heterocycles that are being reported for their potential pharmacological profile. Efforts have been made in search or novel derivatives with improved biological activity, which include novel synthetic strategies. Owing to the importance Read More

In the post-genomic era, more and more interests have been focusing on epigenetics. The histones studded with certain post-translational modifications (PTMs) are becoming one of the cores in protein chemical biology research. The biological generations and functions of these “histone codes”, such as their structural diversity, sophisticated regulations and complex cross-talks, are gradually discovered but still w Read More

A highly efficient method for synthesis of multifunctionalized benzenes by one-pot multicomponent condensation between malononitrile, substituted aldehyde and cycloheptanone catalyzed by Zn-VCO3 hydrotalcite is reported. With water as solvent, this green chemistry reaction entails mild conditions. It is atom-efficient, high-yielding and pertinent to an extensive variety of multicomponent reactions.

Highly efficient, synthetic procedure for bis-(α-hydroxyalkyl)phosphinic acids is described using N-O-bis( trimethylsilyl)acetamide (BSA). Various substituted aldehydes undergo the addition of hypophosphorous acid in good to excellent yields. Operational simplicity, high yield and shorter reaction time are the key features associated with this protocol.

We report a simplified protocol for the routine direct chemoselective preparation of various piperazines substituted in the 1-position by an electron withdrawing group. These syntheses are based on the reaction of piperazine-1- ium cation with different electrophilic reagents such as acyl chlorides, anhydrides, sulfonyl chlorides, carbamoyl chlorides, and nitrourea as well. Piperazine-1-ium cation was chosen because the re Read More

The first total syntheses of salmoxanthin and deepoxysalmoxanthin were accomplished by stereoselective Wittig reaction of a C15-tri-n-butylphosphonium salt bearing a 3,6-dihydroxy-ε-end group with the corresponding C25- apocarotenals. The 3,6-dihydroxy-ε-end moiety was constructed by chemo- and stereoselective reduction of the γ- hydroxy-α,β-cyclohexenone derivative.

A new approach for aminodehalogenation reaction between 3-chloropyrazine-2-carboxamide and ringsubstituted anilines is described. A series of 16 compounds (15 of them novel) derived from pyrazinamide have been synthesized successfully using the advantage of microwave-assisted reaction. The conditions for this aminodehalogenation reaction have been put to investigation to optimize the conversion, yield and time Read More

N-Methyl-D-aspartic acid (NMDA) has significant potential as a drug to treat diabetes, Parkinson’s and Alzheimer’s disease. Consequently, many efforts have been made for synthesis of NMDA, but there exist some flaws yet. In this paper, we report an improved method for Large-Scale Synthesis of optically pure NMDA by Eschweiler–Clarke reaction and deprotection of benzyl by ACE-Cl reagent. The synthesis has been a Read More

A workable method for the preparation of short oligoribonucleotides from commercially available 5´-O-(4,4´- dimethoxytrityl)-2´-O-(tert-butyldimethylsilyl)ribonucleoside 3´-(2-cyanoethyl-N,N-diisopropylphosphoramidite) building blocks on a soluble tetrakis-O-[4-(1,2,3-triazol-1-yl)methylphenyl]pentaerythritol support has been developed. The 3´-terminal nucleoside was attached as a 3´-O-(4-pentynoyl) derivativ Read More

A Knoevenagel one-pot synthesis of 6-amino-4-oxo-8-(2-thienyl)-3-[2-(2-thienyl)vinyl]-4H-pyrimido[2,1- c][1,2,4]triazine-7-carbonitrile 2 via the reaction of 3-amino-6-[2-(2-thienyl)vinyl]-1,2,4-triazin-5(4H)-one 1 with thiophene- 2-carbaldehyde and malononitrile under basic conditions is described. New fused heterotricyclic nitrogen systems, such as pyrimido[5',4':5,6]pyrimido[2,1-c][1,2,4]triazine 5, 7, 9, 12, 13, 20 and py Read More

Highly efficient one-pot solvent-free grinding method was reported for synthesis of chalcones 3a-j, 5a,b, 7 and bis-chalcones 9, 11. Cyclodehydration of bis-chalcones 9, 11 and chalcones 3 with hydrazine derivatives under solvent- free grinding method afforded bis-pyrazolines 12a,b, 13a,b and pyrazoline derivatives 14a-g, respectively. In a similar manner, grinding of bis-chalcones 9, 11 and chalcones 3 with hy Read More