42900-95-8Relevant academic research and scientific papers
Triethylsiloxymethyl-N,N-dimethylamine, Et3SiOCH2NMe2: A Dimethylaminomethylation (Mannich) Reagent for O–H, S–H, P–H and Aromatic C–H Systems
Gonzalez, Paulina E.,Sharma, Hemant K.,Chakrabarty, Sanchita,Metta-Maga?a, Alejandro,Pannell, Keith H.
, p. 5610 - 5616 (2017/10/13)
Triethylsiloxymethylamine, Et3SiOCH2NMe2, readily synthesized in high yield by the hydrosilylation reaction between Et3SiH and DMF, is an excellent (N,N-dimethylamino)methyl transfer agent to a representative range of aliphatic alcohols, thiols, and Ph2PH (E–H) materials. The reactions are almost instantaneous at room temperature in inert solvents and require no activating agents to produce E–CH2NMe2 products in high yields and illustrate the title compound as an excellent addition to the family of organic reagents. For aromatic alcohols, electrophilic substitution of the aromatic ring occurs in high yield. Crystal structures of new materials such as the cholestero–CH2NMe2 derivative, 2–4-[bis(N,N-dimethylamino)methyl]-1-naphthol, and the phosphine oxide derived from Ph2PCH2NMe2 are reported.
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3- yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a highly selective thyroid hormone receptor β agonist in clinical trials for the treatment of dyslipidemia
Kelly, Martha J.,Pietranico-Cole, Sherrie,Larigan, J. Douglas,Haynes, Nancy-Ellen,Reynolds, Charles H.,Scott, Nathan,Vermeulen, John,Dvorozniak, Mark,Conde-Knape, Karin,Huang, Kuo-Sen,So, Sung-Sau,Thakkar, Kshitij,Qian, Yimin,Banner, Bruce,Mennona, Frank,Danzi, Sara,Klein, Irwin,Taub, Rebecca,Tilley, Jefferson
supporting information, p. 3912 - 3923 (2014/06/09)
The beneficial effects of thyroid hormone (TH) on lipid levels are primarily due to its action at the thyroid hormone receptor β (THR-β) in the liver, while adverse effects, including cardiac effects, are mediated by thyroid hormone receptor α (THR-α). A pyridazinone series has been identified that is significantly more THR-β selective than earlier analogues. Optimization of this series by the addition of a cyanoazauracil substituent improved both the potency and selectivity and led to MGL-3196 (53), which is 28-fold selective for THR-β over THR-α in a functional assay. Compound 53 showed outstanding safety in a rat heart model and was efficacious in a preclinical model at doses that showed no impact on the central thyroid axis. In reported studies in healthy volunteers, 53 exhibited an excellent safety profile and decreased LDL cholesterol (LDL-C) and triglycerides (TG) at once daily oral doses of 50 mg or higher given for 2 weeks.
Oxidative ortho-amino-methylation of phenols via C-H and C-C bond cleavage
Sun, Wenbo,Lin, Huacan,Zhou, Wenyu,Li, Zigang
, p. 7491 - 7494 (2014/02/14)
Initiated by CCl3Br, phenols undergo efficient ortho-selective oxidative cross dehydrogenative coupling (CDC) with trimethylamine. When tetramethylethylenediamine (TMEDA) is used instead of trimethylamine, oxidative carbon-carbon activation coupling (CAC) could occur to give the same salicylamines together with CDC by-products. These reactions are accelerated by a gold salt.
PYRIDAZINONE DERIVATIVES AS THYROID HORMONE RECEPTOR AGONISTS
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Page/Page column 61, (2008/06/13)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.
Synthesis and study of the antiradical activity of substituted hydroxybenzylamines and their hydrogen chloride salts
Dyubchenko,Nikulina,Terakh,Kandalintseva,Markov,Grigor'Ev,Prosenko
, p. 330 - 334 (2007/10/03)
Different alkylated hydroxybenzylamines and their hydrogen chloride salts were synthesized. The rate constants of their reactions with peroxide radicals k1 and the stoichiometric factors of inhibition f were measured in the initiated oxidation of cumene and methyl oleate. Copyright
Method for treating multiple sclerosis
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, (2008/06/13)
Provided is a method of treating multiple sclerosis employing certain phenol and benzamide compounds.
Method of treating inflammatory bowel disease
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, (2008/06/13)
Provided is a method for treating inflammatory bowel disease in mammals utilizing certain phenol and benzamide compounds.
Heterocyclic Spirocyclohexadienones from Substituted Phenols
Moehrle, H.,Schake, D.
, p. 1859 - 1868 (2007/10/03)
Mannich bases were prepared from substituted phenols with aliphatic amines and formaldehyde.Amine exchange with N-methyl-2-naphthylamine followed by a Hofmann Martius rearrangement gave rise to o,o'-amino-hydroxy-diphenylmethane derivatives.Under cyclization conditions some of these compounds produced spirocyclohexadienones, which are the ipso analogs to the hypothetic intermediates postulated in the aminomethylation mechanism of phenols. - Keywords: Mannich Reaction; Phenol Dienone Tautomerism; Hofmann Martius Rearrangement
Method of treating type I diabetes
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, (2008/06/13)
Provided is a method for treating Type I diabetes in mammals utilizing certain phenol and benzamide compounds.
Method for treating inflammation
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, (2008/06/13)
Provided are methods of treating inflammation, arthritis and muscular dystrophy and preventing ischemia-induced cell damage employing certain phenol and benzamide compounds.
