Efficient Synthesis of DNA Containing the Guanine Oxidation-Nitration Product 5-Guanidino-4-nitroimidazole:  Generation by a Postsynthetic Substitution Reaction

2004 ◽  
Vol 6 (2) ◽  
pp. 245-248 ◽  
Author(s):  
William L. Neeley ◽  
Paul T. Henderson ◽  
John M. Essigmann
Keyword(s):  
Substitution Reaction ◽  
Efficient Synthesis ◽  
Guanine Oxidation ◽  
Nitration Product ◽  
Postsynthetic Substitution

The Versatility of the Aryne–Imine–Aryne Coupling for the ­Synthesis of Acridinium Photocatalysts

Synlett ◽  
2021 ◽  
Author(s):  
Christof Sparr ◽  
Valeriia Hutskalova
Keyword(s):  
Substitution Reaction ◽  
Precious Metal ◽  
Photophysical Properties ◽  
Cation Radical ◽  
Coupling Reaction ◽  
Nucleophilic Aromatic Substitution ◽  
The Novel ◽  
Aromatic Substitution ◽  
Efficient Synthesis

AbstractThe increasing use of acridinium photocatalysts as sustainable alternative to precious metal-based counterparts encourages the design and efficient synthesis of distinct catalyst structures. Herein, we report our exploration of the scope of the aryne–imine–aryne coupling reaction combined with a subsequent acridane oxidation for a short two-step approach towards various acridinium salts. The photophysical properties of the novel photocatalysts were investigated and the practical value was demonstrated by a cation-radical accelerated nucleophilic aromatic substitution reaction.

Efficient Synthesis of O-glycosyl-5′-H-Phosphonate Diesters of d4T

2013 ◽  
Vol 483 ◽  
pp. 92-95
Author(s):  
Guo Dong Liu ◽  
Shan Shan Gong ◽  
Si Liu ◽  
Qi Sun
Keyword(s):  
Substitution Reaction ◽  
Efficient Synthesis ◽  
One Pot

A novel and one-pot route for the synthesis ofO-glycosyl-5′-H-phosphonate diesters of d4T has been developed. This analogs were synthesized by controlling tandem substitution reaction on PCl3with 2,6-lutidine as suitable base.

Cobalt(III) Complexes with 4-Methyldiethylene-triamine[2,2'-Methyliminodi(ethylamine)]: Their Separation, Characterization and Reactions

1979 ◽  
Vol 32 (3) ◽  
pp. 519 ◽  
Author(s):  
GH Searle ◽  
SF Lincoln ◽  
SG Teague ◽  
DG Rowe
Keyword(s):  
Catalytic Activity ◽  
Cation Exchange ◽  
Substitution Reaction ◽  
Exchange Resin ◽  
Cation Exchange Resin ◽  
Efficient Synthesis ◽  
Counter Ions ◽  
Visible Spectra ◽  
Oxygen Oxidation

An efficient synthesis of 2,2'-methyliminodi(ethylamine) trihydrochloride (medien,3HCl) from diethylenetriamine (dien) is described. The reactions [CO(NH3)5Cl] C12+2medien, and oxygen-oxidation of cobalt(II)+2medien, with charcoal give only the s-fac isomer of [Co(medien)]3+. A little s-fac-[Co(dien)(medien)]3+ is also always formed, and this arises by demethylation of s-fac-[Co(medien)2]3+ with oxygen on charcoal. The substitution reaction [Co(NH3)5Cl] Cl2 + 1.6 medien + 0.4 dien produces a complicated mixture of s-fac-[Co(medien)2]3+, all three isomers s-fac, u-fac and mer of [Co(dien)(medien)]3+, and all three isomers of [Co(dien)2]3+. A procedure using exchanges of the counter-ions, crystallization, and chromatography on SP-Sephadex cation-exchange resin is described for separating and isolating the products, and pure s-fac-[Co(dien)(medien)] (ClO4)3 is obtained preparatively by this means. From isomerization of this complex in water the pure u-fac and mer [Co(dien)(medien)]3+ isomers are isolated. 13C and 1H N.M.R. and visible spectra of the compounds are reported. The equilibrium isomer proportions of [Co(dien)2]3+, [Co(dien)(medien)]3+ and [Co(medien)2]3+ are discussed. Some particular charcoal samples, which lack catalytic activity towards cobalt(III) equilibrations, effect the unusual conversion of s-fac-[Co(medien)2]3+ into u-fac-[Co(arnam)]3+ (amam = 2,3-bis[(2-aminoethyl)(methyl)amino-ethylimino]-1-methylpiperazine).

Highly Efficient Synthesis of Multi-Substituted Allenes from Propargyl­ Acetates and Organoaluminum Reagents Mediated by Palladium

Synthesis ◽  
2017 ◽  
Vol 49 (16) ◽  
pp. 3643-3653 ◽  
Author(s):  
Qinghan Li ◽  
Zhen Zhang ◽  
Xuebei Shao ◽  
Gang Zhang ◽  
Xinying Li
Keyword(s):  
Efficient Method ◽  
Substitution Reaction ◽  
Efficient Synthesis ◽  
Highly Efficient

A simple and mild catalytic SN2′ substitution reaction of propargyl acetates with organoaluminum reagents is reported. The SN2′ substitution reaction of propargyl acetates with organoaluminum reagents mediated by Pd(PhP3)2Cl2 (1 mol%)/PPh3 (2 mol%)/K2CO3 in tetrahydrofuran at 60 °C for 3–4 hours afforded the corresponding multi-substituted allenes in good yields (up to 94%) with high selectivities (up to 99%). The process was simple and easily performed, which offers an efficient method to synthesize the multi-substituted allene derivatives.

scholarly journals Efficient Synthesis and Docking Analysis of Selective CDK9 Inhibitor NVP-2

2021 ◽  
Vol 03 (02) ◽  
pp. e50-e55
Author(s):  
Abdusaid Saidahmatov ◽  
Xue-Wu Liang ◽  
Yu-Qiang Shi ◽  
Xu Han ◽  
Hong Liu
Keyword(s):  
Substitution Reaction ◽  
Binding Mode ◽  
Synthesis Process ◽  
Cyclin Dependent Kinase ◽  
Efficient Synthesis ◽  
Reaction Conditions ◽  
Docking Analysis ◽  
Microwave Reaction ◽  
Design Ideas ◽  
Harsh Conditions

Graphical AbstractNVP-2 (1), a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9), showed potent antitumor activity in preclinical studies. In this work, we designed and adopted a convergent synthetic route to efficiently synthesize NVP-2 (1). The key intermediate (7) was synthesized from malononitrile (2) and 1-bromo-2-(2-bromoethoxy)ethane (3) by successive cyclization, reduction, nucleophilic substitution with 2-bromo-6-fluoropyridine, and Suzuki–Miyaura reaction with (5-chloro-2-fluoropyridin-4-yl)boronic acid. Another key intermediate (11) was synthesized from (S)-1-methoxypropan-2-ol (8) by reaction with TsCl, electrophilic substitution reaction with tert-butyl ((1r,4r)-4-aminocyclohexyl)carbamate, and then by deprotection of Boc. Finally, a substitution reaction by the key intermediates (7) and (11) to afford the target product NVP-2 (1). The reaction conditions of the whole synthesis process were simple and mild, free of harsh conditions such as the microwave reaction and dangerous reagents in the original patent, and realized the efficient synthesis of NVP-2. In addition, we analyzed the binding mode of NVP-2 in the active pocket of CDK9 to provide reasonable design ideas for subsequent discovery of novel CDK9 inhibitors.

VCl3 Catalysed Efficient Synthesis of Bis(indolyl)methanes

2005 ◽  
Vol 2005 (4) ◽  
pp. 222-223 ◽  
Author(s):  
Bavanthula Rajitha ◽  
Penthala Narsimha Reddy ◽  
Buridapad Sunil Kumar ◽  
Neeladri Sreenivasulu ◽  
Yerram Reddy Thirupathi Reddy
Keyword(s):  
Substitution Reaction ◽  
Electrophilic Substitution ◽  
Room Temperature ◽  
Aromatic Aldehydes ◽  
Electrophilic Substitution Reaction ◽  
Efficient Synthesis

VCl3 is found to be an efficient catalysts for the electrophilic substitution reaction of indoles with aromatic aldehydes in dichloromethane to afford the corresponding bis(indolyl)methanes in excellent yields at room temperature.

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