Design and Synthesis of Some New Biologically Active Indeno[1,2-c]pyrazolones

Russian Journal of General Chemistry - The reaction between different arylhydrazones and ninhydrin (= indene-1,2-3-trione) in acetonitrile at room temperature is described to produce novel...     

Facile Synthesis of Biologically Active Peptides Using Phase Transfer Reagents as C-Terminal Protecting Group

Phase-transfer reagents (basic, neutral, and acidic) can temporarily protect carboxyl groups by salt formation of C-terminal free amino acids or peptides during peptide synthesis. The salts of amino acids or peptides behave as RNH₂ rather than RNH₃⁺. At least there is a sufficient concentration of the free amine to act as a nucleophile under the reaction conditions. Many biologically active small peptides have been synthesized by this procedure. No racemization was detected. Unusual amino acids such as β-alanine, and ε-aminohexanoic acid can be incorporated into peptides in high yields.     

Reaction of Anthranilonitrile with Some Active Methylene Reagents: Synthesis of Some New Quinoline and Quinazoline Derivatives

Anthranilonitrile (1) reacts with ethyl cyanoacetate and its dimer, malononitrile, cyanothioacetamide and N‐arylidene cyanoacetohydrazides 12a–c to afford pyrano[2,3‐b]quinoline 5, cyanomethyl‐quinazoline 10, pyrazolo[2,3‐a]quinazoline 12 and triazolo[4,3‐a]‐quinoline derivatives 16a–c, respectively. Structures and conceivable mechanisms are discussed.     

Novel Organophosphorus Reagents for the Synthesis of Amines

Abstract:

New organophosphorus equivalents of a² type N-protected amine synthons are presented.     

Synthesis of Some New Biologically Active Sulfur Compounds Containing Pyrazolo[3,4-d] pyrimidine Moiety

A novel series of the pyrazolo[3,4-d]pyrimidines having biologically active sulfur moieties 3-20 were prepared via reaction of 4-mercapto-1-phenyl-1 H -pyrazolo[3,4-d]pyrimidine 3 with different reagents. Identification of the new compounds was established by elemental analyses, IR, 1 H-NMR, and mass spectral data. Some of the obtained compounds showed the interesting antimicrobial activity comparable to antibiotic chloramphenicol as standard antibacterial agent and Terbinafin as a standard antifungal agent.     

Synthesis of Some New Spiro Heterocycles from the Reaction of Cycloalkylidenemal Ononitriles with Active Methylene Reagents

The reaction of cycloalkylidenemalononitriles 1a–c with some active methylene reagents as well as cycloalkanones in boiling ethanol containing piperidine catalyst affords a series of new spiro heterocyclic systems.     

Synthesis of Some Biologically Active Pyrazole, Thiazolidinone, and Azetidinone Derivatives

Pyrazole, thiazolidinone, and azetidinone derivatives were synthesized from chalcones of 4-hydroxycoumarin. The structures of all the synthesized compounds were confirmed on the basis of spectral and analytical data. The compounds were screened in vitro for their antibacterial activity against various bacterial strains.     

Synthesis of Biologically Active 1-Arylethylphosphonates

A convenient and inexpensive general preparation method for 1-arylethylphosphonic acids and their esters was developed involving in reduction of the corresponding 1-ethenylphosphonates by ammonium formate in the presence of palladium on carbon. A homogeneous enantioselective hydrogenation of 1-arylethenylphosphonic acids in the presence of chiral ruthenium catalysts provided optically active 1-arylethylphosphonic acids of enantiomeric purity up to 86%. The preliminary data on biological activity testing of the 1-arylethylphosphoic acids synthesized evidence that some among the compounds obtained are low-toxic substances with the properties of immunosuppressors of the central type of action.     

具有生物活性的有机磷化合物研究：IX.甘氨酰胺的硫代磷酰化衍生物的合…

通过硫代磷酰－氯酯Ｎ，Ｎ－二丙基－α－乙氨基乙酰胺反应合成了２１种α－硫代磷酰基胺基乙酰胺衍生物，所合成的化合物用元素分析，ＨＮＭＲ和Ｐ ＮＭＲ进行了表征，并进行了杀虫和杀螨活性的试验。     

One-Pot Synthesis of New,Biologically Active 3,5-Disubstituted-1,2,4-oxadiazoles

New chiral 3,5-disubstituted-1,2,4-oxadiazoles have been prepared via an efficient one-pot procedure by the condensation of new chiral amidoximes derived from amino acids with aldehydes. This method is applicable to both aliphatic and aromatic aldehydes, leading easily to the corresponding pure oxadiazoles in excellent yields. These new compounds were tested for their antibacterial and antifungal activities using microdilution tests against some strains of bacteria and fungi, and they showed excellent antibacterial activity.     

α-Ferrocenylalkylation of Some Biologically Active Compounds

Russian Journal of Organic Chemistry -     

Synthesis of Biologically Active Carvacrol Compounds using Different Solvents and Supports

Natural monoterpenoids have been documented for their acute toxicity and repellent, antifeedent, reproduction inhibitory, and insecticidal actions. The present work aims to derive a variety of ether and ester compounds using polymer‐supported reactions from the polymer‐supported carvacrol anion was reacted with alkyl halides and acid chlorides to afford carvacryl ethers and esters, respectively. Furthermore, a special study on the effect of different solvents and supports revealed that Amberlite IRA 400 (chloride form) was found to be the best polymer support and acetone among the solvents.     

Synthesis and Some Characteristics of Magnetic Matrices for Fixation of Biologically Active Substances

A possibility of production of nonporous magnetic matrices with two-layer coating based on cobalt ferrite with the aim to use these matrices for fixation of biologically active substances was considered. The function of the first layer (silica coating) is to shield the cobalt ferrite surface and provide conditions for applying the second (polymer) layer containing various functional groups.     

Phosphonate-Mediated Synthesis of Biologically Active Cyclopentanones and Cyclopentenones

The synthesis and reactivity of 3-(phosphorylmethyl)cyclopent-2-enones as well as a complete desymmetrization of meso -tartaric acid are discussed as a platform for developing the synthesis of racemic rosaprostol and enantiomeric forms of prostaglandin B 1 methyl ester, isoterrein, and neplanocin A.     

New Synthetic Methodology and Biologically Active Substances

The η⁵-cyclopentadienyl-η²-propenealkylnickel complexes 4–9 (alkyl  CH₃, CD₃, CH₂SiMe₃, CH₂ CH₃, CH₂ CH₂ CH₃ and CH(CH₃)₂) have been prepared by treating nickelocene (1) with the appropriate organomagnesium halides 2a–2f and propene at ?20 to ?10°C. Temperature dependent ¹H-NMR spectra result from rotation of the propene molecule around the nickel—olefin axis; in the case of 4 and 8, two rotamers a and b can be distinguished below ca. ?60°C. The decomposition pathways for 4 and 8 are discussed.     

Synthesis and Radiation Stability of Some New Biologically Active Hydroquinoline and Pyrimido[4,5‐b]quinoline Derivatives

A new series of hydroquinolines 6a‐d, 10, 12, 15, 17b, 20 and pyrimidoquinolines 7, 8, 9a, 11, 14 and 16 were synthesized starting from 2‐amino‐4‐(3‐bromo‐phenyl)‐7,7‐dimethyl‐1‐naphthalen‐1‐yl‐5‐oxo‐1,4,5,6,7,8‐hexahydro‐quinoline‐3‐carbonitrile 6b. The structures of the synthesized compounds were elucidated by elemental analyses and spectral data. Compounds 6a, 10, 11 and 18 exhibited a remarkable antifungal activity compared with fungicide Mycostatine. Radiosterilization of the biologically active compounds 6a, 10 and 11 in the dry state may prove to be applicable [retaining their structures unchanged up to (40 kGy)].