- Pyridine methylamine compound and preparation method thereof
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The invention provides a pyridine methylamine compound and a preparation method thereof. The preparation method comprises the steps that tetrahydrofuran and sodium borohydride are sequentially added into a cyanopyridine compound, then an iodine-containing tetrahydrofuran solution is dropwise added, a reaction is conducted at the temperature of 20-30 DEG C, and after dropwise adding is completed, stirring is carried out continuously; after the reaction is finished, methanol is added for refluxing, extracting and spin-drying are carried out to obtain the pyridine methylamine compound; wherein a functional group in the cyanopyridine compound is selected from chlorine, bromine, methyl, ethyl, amino or hydrogen; according to the preparation method, high-temperature and high-pressure special equipment does not need to be used, so that the preparation method is relatively safe, and dangerous accidents such as explosion and fire disasters are avoided; besides, the preparation method is relatively environment-friendly, recycling treatment of hazardous waste (used Raney nickel) is not involved, the economic benefit is relatively high, borane generated by the synthesis method is converted into boric acid esters in the post-treatment process, the treatment cost is low, and the harm to the environment is much small.
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Paragraph 0110-0116
(2021/08/28)
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- α2-adrenoceptor antagonists: Synthesis, pharmacological evaluation, and molecular modeling investigation of pyridinoguanidine, pyridino-2-aminoimidazoline and their derivatives
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We have previously identified phenylguanidine and phenyl-2-aminoimidazoline compounds as high affinity ligands with conflicting functional activity at the α2-adrenoceptor, a G-protein-coupled receptor with relevance in several neuropsychiatric conditions. In this paper we describe the design, synthesis, and pharmacological evaluation of a new series of pyridine derivatives [para substituted 2- and 3-guanidino and 2- and 3-(2-aminoimidazolino)pyridines, disubstituted 2-guanidinopyridines and N-substituted-2-amino-1,4-dihydroquinazolines] that were found to be antagonists/inverse agonists of the α2-adrenoceptor. Furthermore, the compounds exert their effects at the α2-adrenoceptor both in vitro in human prefrontal cortex tissue and in vivo in rat brain as shown by microdialysis experiments. We also provide a docking study at the α2A- and α2C-adrenoceptor subtypes demonstrating the structural features required for high affinity binding to the receptor.
- Kelly, Brendan,McMullan, Michela,Muguruza, Carolina,Ortega, Jorge E.,Meana, J. Javier,Callado, Luis F.,Rozas, Isabel
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supporting information
p. 963 - 977
(2015/01/30)
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- 2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor
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We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.
- Mochizuki, Akiyoshi,Nagata, Tsutomu,Kanno, Hideyuki,Suzuki, Makoto,Ohta, Toshiharu
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experimental part
p. 1623 - 1642
(2011/04/21)
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- PROKINETICIN 1 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
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Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.
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Page/Page column 29
(2012/01/13)
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- Prokineticin 1 receptor antagonists
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The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.
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Page/Page column 29
(2008/12/04)
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- PROKINETICIN 2 RECEPTOR ANTAGONISTS
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The present invention relates to certain novel compounds of Formula (I): and methods for the treatment of prokineticin 2 or prokinetin 2 receptor mediated disorders.
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Page/Page column 84
(2010/11/28)
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