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Fragments

NEWS

June 25, 2019

June 25, 2019

Enamine’s covalent fragments
produce potent and unique hits

In a recent JACS paper several academic groups collaborated on discovery of novel covalent inhibitors using a library of 993 acrylamides and chloroacetamides sourced from Enamine’s covalent fragment collection. The design was focusing on mild electrophiles that were supposed to overcome the selectivity challenge. The library was characterized by a new high-throughput thiol-reactivity assay and screened against 10 cysteine-containing proteins. Potent and unique primary hits have been found in the majority (7 out of 10) of cases.

A refined library used in the research with a few frequent hitters and excessively reactive fragments removed is available from Enamine on request >

Ref.: J. Am. Chem. Soc. 2019, 141, 8951−8968

Reach out to new chemical space breaking the availability bias:
11 000 000 000 molecules and beyond

REAL compounds

NEWS

June 24, 2019

June 24, 2019

Atomwise and Enamine to Advance Pediatric Oncology With the World’s First and Largest Ten Billion Compound Virtual Screen

10 Billion REAL compounds will be searched using AI powered drug screening platform to find novel small molecules for the treatment of pediatric cancers. In collaboration with academic researchers, Atomwise and Enamine said the “10-to-the-10 program” will seek to maximize the opportunity to develop drugs for new target proteins to inhibit cancer growth and metastasis. Read PRESS RELEASE >

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ADME/T & in-vivo PK

Scientific research and development of techniques for the synthesis of organic compounds

High Fidelity Fragments

High Fidelity Library

Fragments of high MedChem tractability  

MedChem Highlights

Analogues of CF3-Pyridine for Drug Design

REAL Database

The largest enumerated database of synthetically feasible molecules

Functional Compounds

Impurity Reference Standards
 

Covalent Fragments

Covalent Fragments

Diverse covalent warheads with balanced reactivity

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MedChem Highlights

2 000 new building blocks are synthesized monthly. Here is an important update to our MedChem Highlights from June 2019

Sugar-like Building blocks
Heterocyclic scaffolds
Morpholine Bioisosteres
Analogues of CF3-Pyridine for Drug Design
Oxetanes
Sulfoximines
P(O)Me2-containing BBs

Recent News

  • 25 June 2019   News

    Enamine’s covalent fragments produce potent and unique hits

    In a recent JACS paper several academic groups collaborated on discovery of novel covalent inhibitors using a library of 993 acrylamides and chloroacetamides sourced from Enamine’s covalent fragment collection. The design was focusing on mild electrophiles that were supposed to overcome the selectivity challenge. The library was characterized by a new high-throughput thiol-reactivity assay and screened against 10 cysteine-containing proteins. Potent and unique primary hits have been found in the majority (7 out of 10) of cases.

  • 24 June 2019   Press Releases

    Atomwise and Enamine to Advance Pediatric Oncology With the ...

    Atomwise, Enamine, and top university researchers collaborate to discovery novel small molecules for the treatment of pediatric cancers using the power of AI and novel chemistry.

    Read press release

  • 26 March 2019   Press Releases

    Enamine extends multi-year drug discovery collaboration with Lundbeck

    Enamine and H. Lundbeck A/S (Lundbeck) announced the expansion of their research collaboration. Enamine will support Lundbeck’s in-house discovery chemistry competencies with three principal assets enabling Lundbeck to optimally identify and develop hit series in its multiple research programs. A large diverse library of 100 000 new screening compounds was done for hit finding activities on numerous therapeutic targets. Enamine’s make-on-demand REAL compounds are for efficient access to billions of novel chemical compounds. Enamine FTE increased dedicated team of chemists to effectively support Lundbeck on all hit related follow-up activities backed by immediate access to over 170 000 building blocks in Enamine’s inventory.

    Read press release

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The publications listed below are the result of a creative joint work of Enamine chemists and our cooperation partners at ChemBioCenter, The Institute of High Technologies, The Institute of Organic Chemistry and Karlsruhe Institute of Technology (KIT).

One-Pot Parallel Synthesis of Alkyl Sulfides, Sulfoxides, and Sulfones
Bogolubsky, A. V.; Moroz, Y. S.; Mykhailiuk, P. K.; Ostapchuk, E. N.; Rudnichenko, A. V.; Dmytriv, Y. V.; Bondar, A. N.; Zaporozhets, O. A.; Pipko, S. E.; Doroschuk, R. A.; Babichenko, L. N.; Konovets, A. I.; Tolmachev, A.
ACS Comb. Sci. 2015, in press


Synthesis and studies on gem-fluorinated 2-azabicyclo[n.1.0]alkanes
Kubyshkin, V.; Kheylik, Y.; Mykhailiuk, P. K.
J. Fluorine Chem. 2015, in press


Design, Synthesis, and Characterization of SO2 -Containing Azabicyclo[3.n.1]alkanes: Promising Building Blocks for Drug Discovery
Druzhenko, T.; Denisenko, O.; Kheylik, Y.; Zozulya, S.; Shishkina, S. S.; Tolmachev, A.; Mykhailiuk, P. K.
Org. Lett. 2015, in press


Synthesis and Structural Analysis of Angular Monoprotected Diamines Based on Spiro[3.3]heptane Scaffold
Chernykh, A. V.; Radchenko, D. S.; Grygorenko, O. O.; Daniliuc, C. G.; Volochnyuk, D. M.; Komarov, I. V.
J. Org. Chem. 2015, in press


Synthesis of Trifluoromethyl-Containing Polysubstituted Aromatic Compounds by Diels–Alder Reaction of Ethyl 3-Benz­amido-2-oxo-6-(trifluoromethyl)-2H-pyran-5-carboxylate
Kondratov, I. S.; Tolmachova, N. A.; Dolovanyuk, V. G.; Gerus, I. I.; Daniliuc, C-G.; Haufe, G.
Eur. J. Org. Chem. 2015, in press


γ-(S)-Trifluoromethyl proline: Evaluation as a structural substitute of proline for solid state 19F-NMR peptide studies
Kubyshkin, V. S.; Afonin, S.; Kara, S.; Budisa, N.; Mykhailiuk P. K.; Ulrich, A. S.
Org. Biomol. Chem. 2015, in press


Synthesis of a 2,5-Diazabicyclo[2.2.1]heptane-Derived α,β-Diamino Acid
Ivon, Y. M.; Tymtsunik, A. V.; Komarov, I. V.; Shishkin, O. V.; Grygorenko, O. O.
Synthesis 2015, in press


Arylation of perfluoroalkyl vinyl sulfoxides via the Heck reaction
Sokolenko, L. V.; Yagupolskii, Y. L.; Vlasenko, Y. G.; Babichenko, L. N.; Lipetskij, V. O.; Anselmi, E.; Magnier, E.
Tetrahedron Lett. 2015, in press


Delivery of SiC-based nanoparticles into live cells driven by cell-penetrating peptides SAP and SAP-E
Serdiuk, T.; Bakanovich, I.; Lysenko, V.; Alekseev, S. A.; Skryshevsky, V. A.; Afonin, S.; Berger, E.; Géloëna, A.; Komarov, I. V.
RSC Adv. 2015, 5, 20498-20502


Synthesis of isomeric (3,3,3-trifluoropropyl)anilines
Trofymchuk, S.; Bezdudny, A.; Pustovit, Y.; Mykhailiuk, P. K.
J. Fluorine Chem. 2015, 171, 174–176


Facile one-pot synthesis of 4-substituted semicarbazides
Bogolubsky, A. V.; Moroz, Y. S.; Mykhailiuk, P. K.; Dmytriv, Y. V.; Pipko, S. E.; Babichenko, L. N.; Konovets, A. I.; Tolmachev, A.
RSC Adv. 2015, 5, 1063-1069


The Most Reactive Amide As a Transition-State Mimic For cis–trans Interconversion
Komarov, I. V.; Yanik, S.; Ishchenko, A. Yu.; Davies, J. E.; Goodman, J. M.; Kirby A. J.
J. Am. Chem. Soc. 2015, 137 (2), 926–930


Design and Synthesis of Novel 19F-Amino Acid: A Promising 19F NMR Label for Peptide Studies
Bandak, D.; Babii, O.; Vasiuta, R.; Komarov, I. V.; Mykhailiuk, P. K.
Org. Lett. 2015, 17 (2), 226–229


Multigram Synthesis of Fluoroalkyl-Substituted Pyrazole-4-carboxylic Acids
Iminov, R. T.; Mashkov, A. V.; Vyzir, I. I.; Chalyk, B. A.; Tverdokhlebov, A. V.; Mykhailiuk, P. K.; Babichenko, L. N.; Tolmachev, A. A.; Volovenko, Y. M.; Biitseva, A.; Shishkin, O. V.; Shishkina, S. V.
Eur. J. Org. Chem. 2015, 4, 886–891


An Expedient and Practical Approach to Functionalized 3-Aza-, 3-Oxa-, and 3-Thiabicyclo[3.3.1]nonane Systems
Ishchenko, A. Y.; Yanik, S.; Rusanov, E. B.; Komarov, I. V.; Kirby, A. J.
Synthesis 2015, 47(03), 367


2014

Synthesis of Thieno[2,3-d]imidazoles by Copper-Catalyzed Amidine Cyclization
Liubchak, K.; Tolmachev, A.; Nazarenko, K.
Synlett 2014, 25(07), 965-968


Three-Component Synthesis of 4-Aroyl-2(1),4,5,7-Tetrahydropyrazolo[3,4-b]Pyridin-6-Ones and Their Properties
Petrova, O. N.; Zamigajlo, L. L.; Gella, I. M.; Musatov, V. I.; Shishkina, S. V.; Shishkin, O. V.; Vashchenko, E. V.; Borisov, A. V.; Lipson, V. V.
Chemistry of Heterocyclic Compounds 2014, 50(4), 514-527


Role of Protein Phosphatase 1 in Dephosphorylation of Ebola Virus VP30 Protein and Its Targeting for the Inhibition of Viral Transcription
Ilinykh, P. A.; Tigabu, B.; Ivanov, A.; Ammosova, T.; Obukhov, Y.; Garron, T.; Kumari, N.; Kovalskyy, D.; Platonov, M. O.; Naumchik, V. S.; Freiberg, A. N.; Nekhai, S.; Bukreyev, A.
The Journal of Biological Chemistry, 2014, 289, 22723-22738


Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core
Sarnpitak. P.; Mujumdar, P.; Morisseau, C.; Hwang S.H.; Hammock, B; Iurchenko, V.; Zozulya, S.; Gavalas, A.; Geronikaki, A.; Ivanenkov, Y.; Krasavin, M.
Eur J Med Chem., 2014, 84, 160-172


Synthesis of pyrazoline-thiazolidinone hybrids with trypanocidal activity
Havrylyuk, D.; Zimenkovsky, B.; Karpenko, O.; Grellier, P.; Lesyk, R.
Eur J Med Chem., 2014, 85, 245–254


1E7-03, a low MW compound targeting host protein phosphatase-1, inhibits HIV-1 transcription
Ammosova, T.; Platonov, M,; Ivanov, A.; Saygide?er Kont, Y.; Kumari, N.; Kehn-Hall, K.; Jerebtsova, M.; Kulkarni, A. A.; Üren, A.; Kovalskyy, D.; Nekhai, S.
British Journal of Pharmacology, 2014, 171 (22), 5059-5075


How Accurately Can We Predict the Melting Points of Drug-like Compounds?
Tetko, I. V.; Sushko, Y.; Novotarskyi, S.; Patiny, L.; Kondratov, I.; Petrenko, A. E.; Charochkina, L.; Asiri, A. M.
J. Chem. Inf. Model., 2014, 54 (12), 3320–3329


Enzyme-Catalyzed Kinetic Resolution of 2,2,2-Trifluoro-1-(heteroaryl)ethanols: Experimental and Docking Studies
Kucher, O. V.; Kolodiazhnaya, A. O.; Smolii, O. B.; Prisuazhnyk, D. V.; Tolmacheva, K. A.; Zaporozhets, O. A.; Moroz, Y. S.; Mykhailiuk, P. K.; Tolmachev, A.A.
Eur. J. Org. Chem. 2014, 34, 7692–7698


Synthesis of Boc-protected 4,5-methano-β-proline
Tymtsunik, A. V.; Ivon, Y. M.; Komarov, I. V.; Grygorenko, O. O.
Tetrahedron Lett. 2014, 55 (22), 3312–3315


A one-pot parallel reductive amination of aldehydes with heteroaromatic amines
Bogolubsky, A. V.; Moroz, Y. S.; Mykhailiuk, P. K.; Panov, D. M.; Pipko, S. E.; Konovets, A. I.; Tolmachev, A.
ACS Comb. Sci. 2014, 16 (8), 375–380


Structure Analysis and Conformational Transitions of the Cell Penetrating Peptide Transportan 10 in the Membrane-Bound State
Fanghänel, S.; Wadhwani, P.; Strandberg, E.; Verdurmen, W. P. R.; Bürck, J.; Ehni, S.; Mykhailiuk, P. K.; Afonin, S.; Gerthsen, D.; Komarov, I. V.; Brock, R.; Ulrich, A. S.
PLOS ONE 2014, 9, 1-14

Design and Synthesis of a Monofluoro-Substituted Aromatic Amino Acid as a Conformationally Restricted 19F NMR ­Label for Membrane-Bound Peptides
Tkachenko, A. N.; Mykhailiuk, P. K.; Radchenko, D. S.; Babii, O.; Afonin, S.; Ulrich, A. S.; Komarov, I. V.
Eur. J. Org. Chem. 2014, 17, 3584-3591


Synthesis of Trifluoromethyl-Substituted 3-Azabicyclo[n.1.0]alkanes: Advanced Building Blocks for Drug Discovery
Artamonov, O. S.; Slobodyanyuk, E. Y.; Volochnyuk, D. M.; Komarov, I. V.; Tolmachev, A. A.; Mykhailiuk, P. K.
Eur. J. Org. Chem. 2014, 17, 3592-3598


One-pot parallel synthesis approach to secondary amines based on the reductive amination of ketones
Bogolubsky, A. V.; Moroz, Y. S.; Pipko, S. E.; Panov, D. M.; Konovets, A. I.; Doroschuk, R.; Tolmachev, A.
Synthesis 2014, 46(13), 1765-1772


Toward Lead-Oriented Synthesis: One-Pot Version of Castagnoli Condensation with Nonactivated Alicyclic Anhydrides
Ryabukhin, S. V.; Panov, D. M.; Granat, D. S.; Ostapchuk, E. N.; Kryvoruchko, D. V.; Grygorenko, O. O.
ACS Comb. Sci. 2014, 16 (3), 146–153


Bis(2,2,2-trifluoroethyl) carbonate as a condensing agent in one-pot, parallel synthesis of unsymmetrical aliphatic ureas
Bogolubsky, A. V.; Moroz, Y. S.; Mykhailiuk, P. K.; Granat, D. S.; Pipko, S. E.; Konovets, A. I.; Doroschuk, R.; Tolmachev, A.
ACS Comb. Sci. 2014, 16(6), 303-308


Synthesis and Functionalization of 3-Azolylquinoxalin-2(1H)-ones
Geraschenko, O. V.; Khodakovskiya, P. V.; Shishkin, O. V.; Tolmachev, A. A.; Mykhailiuk, P. K.
Synthesis 2014, 46(11), 1487-1492


Controlling Biological Activity with Light: Diarylethene-Containing Cyclic Peptidomimetics
Babii, O.; Afonin, S.; Berditsch, M.; Reiβer, S.; Mykhailiuk, P. K.; Kubyshkin, V. S.; Steinbrecher, T.; Ulrich, A. S.; Komarov, I. V.
Angew. Chem. Int. Ed. 2014, 53, 3392–3395


Direct Noncatalytic Electrophilic Trifluoroacetylation of Electron-Rich Pyrazoles
Yarmoliuk, D.V.; Arkhipov, V.V.; Stambirskyi, M.V.; Dmytriv, Y.V.; Shishkin, O.V.; Tolmachev, A.A.; Mykhailiuk, P.K.
Synthesis 2014, 46(9), 1254-1260


Sulfonyl Fluorides as Alternative to Sulfonyl Chlorides in Parallel Synthesis of Aliphatic Sulfonamides
Bogolubsky, A. V.; Moroz, Y. S.; Mykhailiuk, P. K.; Pipko, S. E.; Konovets, A. I.; Sadkova, I. V.; Tolmachev, A.
ACS Comb. Sci. 2014, 16(4), 192-197


Gram-Scale Synthesis of 3,5-Methanonipecotic Acid, a Nonchiral Bicyclic β-Amino Acid
Tymtsunik, A. V.; Bilenko, V. A.; Grygorenko, O. O.; Komarov, I. V.
Synlett 2014, 25(3), 355-358


Conformationally restricted glutamic acid analogues: stereoisomers of 1-aminospiro[3.3]heptane-1,6-dicarboxylic acid
Chernykh, A. V.; Radchenko, D. S.; Grygorenko, O. O.; Volochnyuk, D. M.; Shishkina, S. V.; Shishkind, O. V.; Komarov, I. V.
RSC Adv. 2014, 4, 10894-10902


Synthesis of 1-(pyrrolidin-2-ylmethyl)-1H-azoles and their piperidine-derived homologues
Zhersh, S.; Karpenko, O. V.; Ripenko, V.; Tolmachev, A. A.; Grygorenko, O. O.
Cent. Eur. J. Chem 2014, 12(1), 67-73


Convenient synthesis of enantiopure (R-) and (S-)-3-fluoro-3-aminomethylpyrrolidines
Yarmolchuk, V. S.; Mykhalchuk, V. L.; Mykhailiuk, P. K.
Tetrahedron 2014, 70(18), 3011-3017


Enzymatic resolution of chroman-4-ol and its core analogues with Burkholderia cepacia lipase
Kucher, O. V.; Kolodyazhnaya, A. O.; Smoliib, O. B.; Boiko, A. I.; Kubyshkin, V. S.; Mykhailiuk, P. K.; Tolmachev, A. A.
Tetrahedron: Asymmetry 2014, 25(6-7), 563-567


Conformational behavior of peptides containing residues of 3-azetidinesulfonic (3AzeS) and 4-piperidinemethanesulfonic (4PiMS) acids
Grygorenko, O. O.; Zhersh, S.; Oliinyk, B. V.; Shishkin, O. V.; Tolmachev, A. A.
Tetrahedron: Asymmetry 2014, 25(3), 229–237


2013

Confining the χ space of basic natural amino acids: cyclobutane-derived χ1,χ2-constrained analogues of arginine, lysine and ornithine
Radchenko, D. S.; Michurin, O. M.; Grygorenko, O. O.; Scheinpflug, K.; Dathe, M.; Komarov, I. V.
Tetrahedron 2013, 69, 505–511

1
An approach to dihydroisoindolobenzodiazepinones—three-dimensional molecular frameworks
Yaremenko, A. G.; Shelyakin, V. V.; Volochnyuk, D. M.; Rusanov, E. B.; Grygorenko, O. O.
Tetrahedron Lett., 2013, 54, 1195–1197


Synthesis of New Pyrazolo[1,5-a]pyrimidines by Reaction of β,γ-Unsaturated γ-Alkoxy-α-keto Esters with N-Unsubstituted 5-Aminopyrazoles
Stepaniuk, O. O.; Matviienko, V. O.; Kondratov, I. S.; Vitruk, I. V.; Tolmachev, A. O.
Synthesis, 2013, 45(7), 925-930


Insulin receptor-related receptor as an extracellular pH sensor involved in the regulation of acid–base balance
Petrenko, A. G.; Zozulya, S. A.; Deyev, I. E.; Eladari, D.
Biochim. Biophys. Acta, 2013, 1834, 2170–2175


Development of dimethyl sulfoxide solubility models using 163 000 molecules: using a domain applicability metric to select more reliable predictions
Tetko, I. V.; Novotarskyi, S.; Sushko, I.; Ivanov, V.; Petrenko, A. E.; Dieden, R.; Lebon, F.; Mathieu, B.
J. Chem. Inf. Model., 2013, 53 (8), 1990–2000


Synthesis of imidazo[1,2-a]pyrazine and imidazo[1,2-a]pyrimidine derivatives
Borisov, A. V.; Tolmachev, A. A.; Zavada, O. A.; Zhuravel’, I. A.; Kovalenko, S. N.
Chem. Heterocyc. Compd., 2013, 49, 704-711


Stereochemical effects on the aggregation and biological properties of the fibril-forming peptide [KIGAKI]3 in membranes.
Wadhwani, P.; Reichert, J.; Strandberg, E.; Burck, J.; Misiewicz, J.; Afonin, S.; Heidenreich, N.; Fanghanel, S.; Mykhailiuk, P. K.; Komarov, I. V.; Ulrich A. S.
Phys.Chem.Chem.Phys. 2013, 15, 8962-8971


Design, synthesis and application of a CF3-phenylalanine analogue as a label to study peptides by solid state 19F-NMR.
Tkachenko, A. N.; Radchenko, D. S.; Mykhailiuk, P. K.; Afonin, S.; Ulrich, A. S.; Komarov I. V.
Angew. Chem. Int. Ed. 2013, 125, 6632-6635


Incorporation of labile trans-4,5-difluoromethanoproline into a peptide as a stable label for 19F-NMR structure analysis.
Kubyshkin, V. S.; Mykhailiuk, P. K.; Afonin, S.; Grage, S. L.; Komarov, I. V.; Ulrich A. S.
J. Fluorine Chem. 2013, 152, 136-143


Synthesis and characterization of β-trifluoromethyl-substituted pyrrolidines
Yarmolchuk, V. S.; Shishkin, O. V.; Starova, V. S.; Zaporozhets, O. A.; Kravchuk, O.; Zozulya, S.; Komarov, I. V.; Mykhailiuk P. K.
Eur. J. Org. Chem. 2013, 15, 3086-3093


1-Amino-4,4-difluorocyclohexanecarboxylic acid as a promising building block for drug discovery. Design, synthesis and characterization
Mykhailiuk, P. K.; Starova, V.; Iurchenko, V.; Shishkina, S. V.; Shishkin, O. V.; Zaporozhets O.
Tetrahedron 2013, 20, 4066-4075


An easy synthesis of α-trifluoromethyl-amines from aldehydes or ketones using the Ruppert-Prakash reagent
Radchenko, D. S.; Michurin, O. M.; Chernykh, A. V.; Lukin, O.; Mykhailiuk P. K.
Tetrahedron Lett. 2013, 54, 1897-1898


Synthesis of Isomeric 6-Trifluoromethyl-3-azabicyclo[3.1.0]hexanes: Conformationally Restricted Analogues of 4-Trifluoromethylpiperidine
Artamonov, O. S.; Slobodyanyuk, E. Y.; Shishkin, O. V.; Komarov, I. V.; Mykhailiuk P. K.
Synthesis 2013, 45, 225-230


A 19F NMR Label To Substitute Polar Amino Acids in Peptides: A CF3-Substituted Analogue of Serine and Threonine.
Tkachenko, A. N.; Mykhailiuk, P. K.; Afonin, S.; Radchenko, D. S.; Kubyshkin, V. S.; Ulrich, A. S.; Komarov I. V.
Angew. Chem. Int. Ed. 2013, 52, 1486-1489


Protecting group free synthesis of carboxyl-substituted dihydropyrimidines through Biginelli reaction
Ostapchuk, E.N.; Plaskon, A.S.; Grygorenko, O.O.; Tolmachev, A.A.; Ryabukhin, S.V.
J. Heterocyclic Chem., 2013, 50 (6), 1299-1303


A facile synthesis of functionalized 1,2,6,7-tetrahydroimidazo[1,5-C] pyrimidine-3,5-diones
Lebed, P.S.; Kos, P.O.; Tolmachev, A.; Vovk, M.V.; Boyko, A.N.; Chekotylo, A.
Synthetic Commun., 2013, 43 (17), 2343-2348


A noncatalytic approach to hetaryl-annulated 1,2,4-thiadiazine-1,1-dioxides
Cherepakha, A.; Kovtunenko, V.O.; Tolmachev, A.; Lukin, O.
J. Heterocyclic Chem., 2013, 50 (5), 1071-1077


Synthesis and reactivity of 5-polyfluoroalkyl-5-deazaalloxazines
Dudkin, S.; Iaroshenko, V.O.; Sosnovskikh, V.Y.; Tolmachev, A.A.; Villinger, A.; Langer, P.
Organic and Biomolecular Chemistry, 2013, 11 (32), 5351-5361


A solution-phase parallel synthesis of alkylated guanidines from thioisocyanates and amines
Bogolubsky, A.V.; Grishchenko, A.; Pipko, S.E.; Konovets, A.; Chuprina, A.; Tolmachev, A.; Boyko, A.N.; Chekotylo, A.; Lukin, O.
Mol Diver, 2013, 17 (3), 471-477


Synthesis of 2- and 3-trifluoromethylmorpholines: Useful building blocks for drug discovery
Shcherbatiuk, A.V.; Shyshlyk, O.S.; Yarmoliuk, D.V.; Shishkin, O.V.; Shishkina, S.V.; Starova, V.S.; Zaporozhets, O.A.; Zozulya, S.; Moriev, R., Kravchuk, O.; Manoilenko, O.; Tolmachev, A.A.; Mykhailiuk, P.K.
Tetrahedron, 2013, 69 (19), 3796-3804


A convenient route to 1-alkyl-5-trifluoromethyl-1,2,3-triazole-4-carboxylic acids employing a diazo transfer reaction
Iminov, R.T.; Mashkov, A.V.; Chalyk, B.A.; Mykhailiuk, P.K.; Tverdokhlebov, A.V.; Tolmachev, A.A.; Volovenko, Y.M.; Shishkin, O.V.; Shishkina, S.V.
Eur. J. Org. Chem., 2013, (14), 2891-2897


Efficient synthesis of novel thieno[3,2-b]-, [2,3-c]- and [3,2-c]pyridones by Sonogashira coupling of bromothiophenes with terminal alkynes and subsequent intramolecular C-N bond-forming reaction
Iaroshenko, V.O.; Ali, S.; Babar, T.M.; Abbasi, M.S.A.; Sosnovskikh, V.Y.; Villinger, A.; Tolmachev, A.; Langer, P.
Tetrahedron, 2013, 69 (15), 3167-3181


An efficient synthesis of 1-methyl-4,5,6,7-tetrahydro-1 H-pyrrolo[2,3-c]pyridine and its N6-substituted analogues
Nechayev, M.A., Gorobets, N.Y., Kovalenko, S.M., Tolmachev, A.A.
Synthesis (Germany), 2013, 45 (7), 919-924


A facile synthesis of annulated azolo[c][1,2,4]thiadiazine S,S-dioxides
Cherepakha, A.; Kovtunenko, V.O.; Tolmachev, A.
Tetrahedron Lett., 2013, 54 (8), 986-988


Conformational behaviour of peptides containing a 2-pyrrolidinemethanesulfonic acid (2PyMS) residue
Grygorenko, O.O.; Zhersh, S.; Oliinyk, B.V.; Shishkin, O.V.; Tolmachev, A.A.
Organic and Biomolecular Chemistry, 2013, 11 (6), 975-983


Design, synthesis and transformation of some heteroannulated 3-aminopyridines - Purine isosteres with exocyclic nitrogen atom
Iaroshenko, V.O.; Vilches-Herrera, M.; Gevorgyan, A.; Mkrtchyan, S.; Arakelyan, K.; Ostrovskyi, D.; Abbasi, M.S.A.; Supe, L.; Hakobyan, A.; Villinger, A.; Volochnyuk, D.M.; Tolmachev, A.
Tetrahedron, 2013, 69 (3), 1217-1228


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