- Iron-promoted sulfur sequestration for the substituent-dependent regioselective synthesis of tetrazoles and guanidines
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We have established a facile and versatile synthetic methodology for the construction of tetrazoles and guanidines in the presence of an eco-friendly, inexpensive, easily available iron reagent. Aromatic thioureas with electron-donating substituents produced their respective target products in quantitative yield. In contrast, when electron-withdrawing substituted aromatic thioureas were used, the expected products were obtained in reduced yield. However, the desired products were obtained in good yield at moderate temperature. In addition, mechanistic studies revealed that the synthetic route involved iron-based subsequent reactions of addition and removal of sulfur.
- Pendem, Venkata Bhavanarushi,Tamminana, Ramana,Nannapaneni, Madhavi
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p. 499 - 509
(2021/04/09)
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- Direct guanylation of amino groups by cyanamide in water: Catalytic generation and activation of unsubstituted carbodiimide by scandium(iii) triflate
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Guanylation proceeded efficiently upon treatment of the various amines with cyanamide in the presence of catalytic amounts of scandium(III) triflate under mild conditions. The method did not require the guanylation reagents to be preactivated, and the reaction proceeded efficiently in water. The method, therefore, has practical utility for substrates that dissolve only in aqueous solutions, for example, peptides or pharmacologically important compounds. Georg Thieme Verlag Stuttgart New York.
- Tsubokura, Kazuki,Iwata, Takayuki,Taichi, Misako,Kurbangalieva, Almira,Fukase, Koichi,Nakao, Yoichi,Tanaka, Katsunori
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p. 1302 - 1306
(2014/06/10)
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- Synthesis of symmetrical and unsymmetrical N, N ′-diaryl guanidines via copper/N-methylglycine-catalyzed arylation of guanidine nitrate
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CuI/N-methylglycine-catalyzed coupling reaction of guanidine nitrate with both aryl iodides and bromides takes place at 70-100 °C, affording symmetrical N,N′-diaryl guanidines with good to excellent yields. Unsymmetrical N,N′-diaryl guanidines can be assembled via monoarylation of guanidine nitrate with aryl iodides bearing a strong electron-withdrawing group and subsequent coupling with another aryl iodide.
- Xing, Hui,Zhang, Ye,Lai, Yisheng,Jiang, Yongwen,Ma, Dawei
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experimental part
p. 5449 - 5453
(2012/08/07)
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- FUSED HETEROCYCLYC INHIBITOR COMPOUNDS
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The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound
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Page/Page column 62
(2010/03/02)
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- Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto
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Compounds having activity as inhibitors of the JNK pathway are disclosed. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 through R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to inhibition of the JNK pathway. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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- Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
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Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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