5496-10-6Relevant academic research and scientific papers
Photoreactive fused aziridinylpiperazines on the background of 4-substituted chalcones and their benzimidazolic analogs
Kotlyar, Volodymyr M.,Kolomoitsev, Oleksii O.,Nikolaievskyi, Dmytro V.,Pedan, Polina I.,Chumak, Andrii Yu,Orlov, Valery D.,Shishkina, Svitlana V.,Doroshenko, Andrey O.
, p. 741 - 746 (2019/01/10)
The reaction of bromo-substituted chalcones with various diamino-compounds leads to the fused heterocyclic products, aziridinylpiperazines, exhibiting photoreactivity in the crystalline state. Crystals of 4-nitrosubstituted compounds of this family change their color from yellowish to deep violet-blue, 4-cyanosubstituted ones – from yellowish to pink at UV irradiation. Discussion on the mechanism of this phototransformation is still in progress, however, several facts points to the free radial nature of the photogenerated colored semi-products stabilized only by crystalline state of the irradiated samples. Formation of a mixture of positional isomers at interaction of bromo-chalcones with asymmetric diamines of aliphatic/alicyclic or aromatic series at synthesis of the title compounds is of significant interest as well.
Synthesis of: N -unsubstituted cycloalkylimines containing a 4 to 8-membered ring
Guillemin, Jean-Claude,Nasraoui, Wafa,Gazzeh, Houda
, p. 5647 - 5650 (2019/05/21)
Primary cycloalkylimines with a 4 to 8-membered ring were synthesized by dehydrocyanation of the corresponding α-aminonitriles on solid potassium hydroxide via a vacuum gas-solid reaction. Imine-enamine tautomerism has been demonstrated at room temperature for the most kinetically stable derivatives.
SYNTHESIS OF N-(HETEROARYL)-PYRROLO[3,2-D]PYRIMIDIN-2-AMINES
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Page/Page column 89; 90, (2018/02/28)
This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
Design and synthesis of certain substituted cycloalkanecarboxamides structurally related to safinamide with anticonvulsant potential
Aboul-Enein, Mohamed N.,El-Azzouny, Aida A.,Maklad, Yousreya A.,Ismail, Mohamed A.,Ismail, Nasser S. M.,Hassan, Rasha M.
, p. 3767 - 3791 (2015/06/08)
A series of novel safinamide derivatives were synthesized and biologically evaluated for their anticonvulsant activity against maximal electroshock seizure assay and subcutaneous pentylenetetrazole (s.c. PTZ) screening test. Compound 13b is the most active derivative in s.c. PTZ screening test with an ED50 value lower than that of safinamide by about tenfold. A molecular modeling study, including fitting to sodium channel blockers 3D-pharmacophore model and docking into a branched-chain aminotransferase enzyme active site were consistent with the in vivo results.
Transamination of a-amino nitriles
Popov,Mokhov,Tankabekyan
, p. 21 - 24 (2014/03/21)
α-Amino nitriles containing a primary amino group undergo transamination with aliphatic and aromatic amines under mild conditions with high yields. A probable reaction mechanism involving intermediate elimination of cyanide ion has been proposed.
Approaches to the construction of substituted 4-amino-1 H -pyrrol-2(5 H)-ones
Zali-Boeini, Hassan,Mobin, Mehdi,Hajibabaei, Khadijeh,Ghani, Maryam
experimental part, p. 5808 - 5812 (2012/07/31)
Fully substituted 4-aminopyrrolones are easily accessed via simple routes starting from imines, ketones, or α-bromophenyl acetonitriles. Imines were reacted with KCN/NH4Cl in aqueous ethanol to produce α-arylamino benzyl cyanides. On the other hand, ketones were transformed to the desired α-amino nitriles using a modified Strecker reaction. Then, α-amino nitrile precursors were allowed to react with a suitable acyl halide to produce the corresponding amides. Further treatment of these amides with ethanolic KOH converted them to highly substituted 4-amino-1H-pyrrol-2(5H)- one derivatives in moderate to excellent yields.
Versatile synthesis of free and N-benzyloxycarbonyl-protected 2,2-disubstituted taurines
Wang, Boyuan,Zhang, Wei,Zhang, Leilei,Du, Da-Ming,Liu, Gang,Xu, Jiaxi
, p. 350 - 355 (2008/09/18)
An effective and versatile method was developed to synthesize N-benzyloxycarbonyl-protected and free 2,2-disubstituted taurines. Several novel 2,2-disubstituted taurines, including aliphatic/aromatic and cyclic/acyclic derivatives, were obtained, which demonstrates the generality of this method. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
NEW GALLIUM BISAMINOTHIOLATE COMPLEXES FOR MYOCARDIAL IMAGING
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Page/Page column 11, (2008/12/08)
The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts thereof; wherein A1, A2 and A3 are the same or different cycloalkyl, wherein at least one of A1, A2 or A3 is substituted. R1 through R6 are independently hydrogen or alkyl, R7 and R8 are independently hydrogen or alkyl and RP is hydrogen or sulfhydryl protecting group. This invention is also directed to complexes, wherein said compounds chelate radioactive metal ions, such as Gallium. The complexes of the rpesent invention are useful as myocardial perfusion imaging agents.
Total syntheses of (±)-massadine and massadine chloride
Su, Shun,Seiple, Ian B.,Young, Ian S.,Baran, Phil S.
supporting information; scheme or table, p. 16490 - 16491 (2009/04/13)
The total syntheses of the complex pyrrole-imidazole alkaloids (±)-massadine and (±)-massadine chloride is described using a carefully orchestrated sequence of manipulations on highly polar and structurally complex intermediates. Key to the completion of this synthetic endeavor was the exploration of a unique and chemoselective method to oxidize unprotected guanidines under aqueous conditions in air. This oxidation has been optimized and applied to a selection of spirocyclic guanidines of varying complexity. Additionally, the 3,7-epi analogues of these interesting natural products have been synthesized and fully characterized. Copyright
Methods and compositions for treating amyloid-related diseases
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Page/Page column 156, (2010/11/24)
Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
