134391-76-7Relevant academic research and scientific papers
Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine
Carroll, F. Ivy,Robinson, T. Philip,Brieaddy, Lawrence E.,Atkinson, Robert N.,Mascarella, S. Wayne,Damaj, M. Imad,Martin, Billy R.,Navarro, Hernán A.
, p. 6383 - 6391 (2007)
Epibatidine analogues 3-5, possessing the pyridine ring fused to the 2,3 position of the 7-azabicyclo[2.2.1]heptane ring, and analogue 8a, possessing a benzene ring fused to the 5,6 position, were synthesized by procedures involving key steps of trapping
CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 117, (2018/04/17)
The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from (II), (III), (IV), and (V), and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild congnitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
Synthetic studies pertaining to the 2,3-pyridyne and 4,5-pyrimidyne
Medina, Jose M.,Jackl, Moritz K.,Susick, Robert B.,Garg, Neil K.
, p. 3629 - 3634 (2016/06/06)
We report synthetic studies pertaining to two heterocyclic aryne intermediates: the 2,3-pyridyne and the 4,5-pyrimidyne. First, a 2,3-pyridyne precursor was readily accessed from 2-pyridone using a known procedure. Subsequently, 2,3-pyridyne generation an
2,3-Pyridyne formation by fluoride induced desilylation-elimination
Walters, Michael A.,Shay, John J.
, p. 3573 - 3579 (2007/10/03)
The formation of 2,3-pyridyne by a desilylation-elimination sequence employing anhydrous CsF is reported.
Preparation of Didehydropyridines from (Trimethylsilyl)pyridines
Effenberger, Franz,Daub, Wolfgang
, p. 2119 - 2125 (2007/10/02)
Halogen-substituted (trimethylsilyl)pyridines 2, 3, 5-7 and trifluoromethylsulfonyloxy-substituted (trimethylsilyl)pyridines 9b, 11b are obtained from 2- and 3-halopyridines 1, 4 or hydroxypyridines 8, 10, and 12.Reactions of the 3- and 2-(trimethylsilyl)pyridines 2, 9b and 11b with bases in the presence of furans 15 give only protodesilylation or hydrolysis products but no indication is found for the formation of a 2,3-didehydropyridine. 3-Bromo-4-(trimethylsilyl)pyridine (5a) reacts with KOCMe3 in the presence of furan (15a) to give a mixture of products from which the isoquinoline derivative 20 and the tert-butoxypyridines 23, 24 are formed by addition to 3,4-didehydropyridine.Under comparable conditions far higher yields of 3,4-didehydropyridines are obtained by treatment of the 3-halo-2,4-bis(trimethylsilyl)pyridines 7 with strong bases. Key Words: Didehydropyridines, synthesis of
