1191240-34-2Relevant academic research and scientific papers
Light-Mediated Formal Radical Deoxyfluorination of Tertiary Alcohols through Selective Single-Electron Oxidation with TEDA2+.
Aguilar Troyano, Francisco José,Ballaschk, Frederic,Jaschinski, Marcel,?zkaya, Yasemin,Gómez-Suárez, Adrián
supporting information, p. 14054 - 14058 (2019/11/11)
The synthesis of tertiary alkyl fluorides through a formal radical deoxyfluorination process is described herein. This light-mediated, catalyst-free methodology is fast and broadly applicable allowing for the preparation of C?F bonds from (hetero)benzylic, propargylic, and non-activated tertiary alcohol derivatives. Preliminary mechanistic studies support that the key step of the reaction is the single-electron oxidation of cesium oxalates—which are readily available from the corresponding tertiary alcohols—with in situ generated TEDA2+. (TEDA: N-(chloromethyl)triethylenediamine), a radical cation derived from Selectfluor.
CCR2 MODULATORS
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Paragraph 0210, (2016/12/07)
Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (I) and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of CCR2 receptors.
Substituted Pyrimidine and Triazine Compounds
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Page/Page column 60, (2010/07/10)
Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.
Substituted Indole Compounds
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Page/Page column 54, (2010/09/07)
Substituted indole compounds corresponding to the formula I: In which R8, R9a, R9b, R10, R11, R200, R210, A, D, T, q, s and t have defined meanings, processes for the preparation thereof, pharmaceutical compositions containing such compounds and the use of substituted indole compounds for the treatment or inhibition of pain and other conditions which are at least partly mediated by Bradykinin 1 receptors (B1R).
SULFONYLATED TETRAHYDROAZOLOPYRAZINES AND THEIR USE AS MEDICINAL PRODUCTS
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Page/Page column 107-108, (2010/09/18)
The present invention relates to sulfonylated tetrahydroazolopyrazines, methods for the preparation thereof, medicinal products containing these compounds and the use of substituted indole compounds for the preparation of medicinal products (Formula I).
SUBSTITUTED SULFONAMIDE COMPOUNDS
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Page/Page column 94-95, (2009/10/30)
Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor
Structure-affinity relationships of a unique nicotinic ligand: N1-dimethyl-N4-phenylpiperazinium iodide (DMPP)
Romanelli,Manetti,Scapecchi,Borea,Dei,Bartolini,Ghelardini,Gualtieri,Guandalini,Varani
, p. 3946 - 3955 (2007/10/03)
DMPP is a well-known nicotinic agonist that does not fit any proposed pharmacophore for nicotinic binding and represents a unique ligand among the hundreds of nicotinic agonists studied in the past decades. A systematic modulation of the chemical structure of DMPP, aimed to establish its structure-affinity relationships, is reported. The research has allowed to identify molecules such as 11c, 13c, 14c, and 28c, with affinities for α4β2 receptors in the low nanomolar range, some 2 orders of magnitude lower than the lead compound. The agonistic properties of the most interesting compounds have been assessed by measuring their analgesic activity on mice (hot-plate test). Another result of the research was the identification of DMPP analogues, such as 3a (Ki = 90 nM) and 14b (Ki = 180 nM), that maintain affinity for the central nicotinic receptor when the ammonium function is changed into an aminic one and are therefore possible leads for drug development in neurodegenerative diseases.
