113118-81-3Relevant articles and documents
Synthesis of (±) [5-3H] N′-nitrosoanatabine, a tobacco-specific nitrosamine
Desai, Dhimant,Lin, Guoying,Morimoto, Hiromi,Williams, Philip G.,El-Bayoumy, Karam,Amin, Shantu
, p. 1133 - 1141 (2002)
Tobacco-specific N′-nitrosamines (TSNA) are a unique class of systemic organ-specific carcinogens. The TSNA are formed by N-nitrosation of nicotine and of the minor tobacco alkaloids after harvesting of tobacco and during smoking. The N-nitrosation of anatabine leads to N′-nitrosoanatabine (NAT; 1-nitroso-1,2,3,4-tetrahydro-2,3′-bipyridyl) which requires in-depth assays in laboratory animals other than the rat. Furthermore, delineation of its tissue distribution and metabolism is needed for structure: activity comparisons with other TSNA and for the assessment of potential human risk from this TSNA. We have, therefore, synthesized (±)[5-3 H]NAT. 5-Bromo-3-pyridine-carboxaldehyde was condensed with ethyl carbamate prior to Diels-Alder reaction with 1,4-butadiene to give the racemic anatabine ring system. Hydrolysis, followed by reduction with LiA1T4 and nitrosation, led to (±) [5-3H]NAT (60% yield, specific activity 266 mCi/mmol, radiochemical purity of > 99%). Copyright
SOLID FORMS OF 1-(5-(3-(7-(3-FLUOROPHENYL)-3H-IMIDAZO[4,5-C]PYRIDIN-2-YL)-1H-PYRAZOLO[3,4-B]PYRIDIN-5-YL)PYRIDIN-3-YL)-N,N-DIMETHYLMETHANAMINE
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, (2021/08/27)
The present application relates to two crystalline polymorphic forms, crystalline methanol, ethanol and tetrahydrofuran solvates and a crystalline hydrate of the compound l-(5-(3-(7-(3-fluorophenyl)-3H- imidazo[4,5-c]pyridin-2-yl)-1H-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3- yl)-N,N-dimethylmethanamine (Ipivivint), to a pharmaceutical composition comprising them and their medical use for the treatment of disorders characterized by the activation of of the Wnt signaling pathway selected from cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis and idiopathic pulmonary fibrosis. Also claimed is a process for the preparation of compounds of Formula (I) by reacting a starting material of Formula (A1) with a compound of Formula (A2).
Method for synthesizing 5-bromopyridine-3-formaldehyde
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Paragraph 0020; 0021; 0038; 0039; 0040; 0041; 0042-0046, (2018/04/02)
The invention belongs to the field of organic synthesis, and particularly relates to a method for synthesizing 5-bromopyridine-3-formaldehyde. In the method, 3,5-dibromopyridine is taken as a material, and tetramethylethylenediamine is taken as a stabilizer, so as to react with a Grignard reagent to prepare a product. The existence of tetramethylethylenediamine reduces the impurities in the product, and improves the yield; the synthesis method has a low requirement on the temperature, can be finished under the condition of 5 to 25 DEG C, saves energy consumption, and is easy to operate; in thesynthesis technology, a simple post-processing method has few steps and high yield, and is suitable for industrial production.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND HAVING INHIBITORY EFFECT ON PRODUCTION OF KYNURENINE
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Paragraph 0189, (2013/03/28)
The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I): (wherein R6 and R7 may be the same or different and each represent a hydrogen atom or the like, R8, R9, R19, and R11 may be the same or different and each represent a hydrogen atom or the like, R1 represents lower alkyl which may be substituted with cycloalkyl, or the like, and R3 represents optionally substituted aryl or an optionally substituted heterocyclic group).
