51551-56-5Relevant academic research and scientific papers
An Efficient Two-Step Preparation of α-, β-, γ- or δ-Amino Acids from 2-Pyrazinones, 2-Hydroxypyrimidines or 2-Pyridones Respectively
Zacharie, Boulos,Abbott, Shaun D.,Baigent, Christopher B.,Doyle, Christopher,Yalagala, Ravi Shekar
, p. 6486 - 6493 (2018/11/23)
A practical and efficient two-step procedure is reported for the preparation of a variety of α-, β-, γ- and δ-amino acids from 2-pyridone, 2-pyrazinone or 2-hydroxypyrimidine and derivatives. The procedure is amenable to scale-up and in most cases no chromatographic purification of the product is required. This approach is useful, especially in the synthesis of amino acids or deuterated amino acids that are not obtained by other methods.
Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents
Humphries, Paul S.,Bersot, Ross,Kincaid, John,Mabery, Eric,McCluskie, Kerryn,Park, Timothy,Renner, Travis,Riegler, Erin,Steinfeld, Tod,Turtle, Eric D.,Wei, Zhi-Liang,Willis, Erik
, p. 293 - 297 (2018/01/04)
A series of novel carbazole-containing amides and ureas were synthesized. A structure–activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the desired pharmacokinetic/pharmacodynamic parameters and the results of efficacy studies in db/db mice, compound 50 was selected for further profiling.
CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS
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Paragraph 0299, (2015/10/28)
The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
Asymmetric Michael Addition Reaction of α-Aryl-Substituted Lactams Catalyzed by Chiral Quaternary Ammonium Salts Derived from Cinchona Alkaloids: A New Short Synthesis of (+)-Mesembrine
Nunokawa, Shiori,Minamisawa, Masamitsu,Nakano, Keiji,Ichikawa, Yoshiyasu,Kotsuki, Hiyoshizo
, p. 2301 - 2305 (2015/09/28)
The enantioselective Michael addition reaction of α-aryl-substituted lactams with electron-deficient olefins was efficiently catalyzed using chiral quaternary ammonium salts derived from cinchona alkaloids. This method was highly useful for the construction of an all-carbon-substituted quaternary carbon stereogenic center at the α-position of lactams in good to high yields and with good enantiomeric excess and could be applied to the short synthesis of (+)-mesembrine.
Catalytic asymmetric allylic alkylation of 3-arylated piperidin-2-ones
Michon, Christophe,Bethegnies, Aurelien,Capet, Frederic,Roussel, Pascal,De Filippis, Arnault,Gomez-Pardo, Domingo,Cossy, Janine,Agbossou-Niedercorn, Francine
supporting information, p. 4979 - 4985 (2013/08/23)
The preparation of optically active lactams from 3-aryl-2-piperidinone is reported. The quaternary carbon stereocentres were formed using palladium-catalysed asymmetric allylic alkylation reactions. The resulting enantioenriched compounds are useful inter
NOVEL COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
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Page/Page column 118-119, (2010/04/27)
The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Influence of ring size on the outcome of sulfide contraction reactions with thiolactams. Isolation of bicyclic ketene S,N-acetals and thioisomuenchnones
Michael, Joseph P.,De Koning, Charles B.,Van der Westhuyzen, Christiaan W.,Fernandes, Manuel A.
, p. 2055 - 2062 (2007/10/03)
Reaction between diethyl bromomalonate and 3-phenylpyrrolidine-2-thione yielded a vinylogous urethane by the Eschenmoser sulfide contraction. However, with 3-substituted piperidine-2-thiones, sulfur was retained in the products, and a range of bicyclic heterocycles, including bicyclic ketene S,N-acetals (2-alkylidene-1,3-thiazolidin-4-ones) and stable thioisomuechnones, was isolated. A novel dimeric ketene S,N-acetal was characterised by X-ray crystallography.
Synthesis of lactams by regioselective reduction of cyclic dicarboximides
Milewska, Maria J.,Bytner, Tomasz,Polonski, Tadeusz
, p. 1485 - 1488 (2007/10/03)
Lactams can be obtained by the monothionation of imides with Lawesson's reagent followed by the desulfurization of resulted monothioimides with Raney nickel.
Drugs comprising 2,3- or 3,4-diphenyl derivatives of γ-nitrile-esters or the cyclization products thereof
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, (2008/06/13)
New drugs comprising 2,3- or 3,4-diphenyl derivatives of γ-nitrile-esters or the products of cyclization of the 2,3-diphenyl derivatives according to the formulae A, B and C are claimed. Process for cyclization of 2,3-diphenyl derivatives of γ-nitrile-esters, new 2,3-diphenyl derivatives of γ-nitrile-esters corresponding to the formulae I to VIII are claimed; new 3,4-diphenyl derivatives of the said esters coresponding to the formulae IX and X, and new 3,4-diphenylpiperidone derivatives corresponding to the specific formulae IX to XXVII are described.
