149281-42-5Relevant articles and documents
Direct synthesis of β-aminoketones from amides via novel sequential nucleophilic substitution/Michael reaction
Gomtsyan, Arthur
, p. 11 - 13 (2000)
(formula presented) The synthesis of β-aminoketones from amides can be achieved in a process consisting of sequential nucleophilic substitution at the carbonyl group by vinylmagnesium bromide followed by Michael reaction after quench of the first reaction
Catalytic Enantioselective Pyridine N-Oxidation
Hsieh, Sheng-Ying,Tang, Yu,Crotti, Simone,Stone, Elizabeth A.,Miller, Scott J.
, p. 18624 - 18629 (2019/11/21)
The catalytic, enantioselective N-oxidation of substituted pyridines is described. The approach is predicated on a biomolecule-inspired catalytic cycle wherein high levels of asymmetric induction are provided by aspartic-acid-containing peptides as the aspartyl side chain shuttles between free acid and peracid forms. Desymmetrizations of bis(pyridine) substrates bearing a remote pro-stereogenic center substituted with a group capable of hydrogen bonding to the catalyst are demonstrated. Our approach presents a new entry into chiral pyridine frameworks in a heterocycle-rich molecular environment. Representative functionalizations of the enantioenriched pyridine N-oxides further document the utility of this approach. Demonstration of the asymmetric N-oxidation in two venerable drug-like scaffolds, Loratadine and Varenicline, show the likely generality of the method for highly variable and distinct chiral environments, while also revealing that the approach is applicable to both pyridines and 1,4-pyrazines.
PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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Page/Page column 130; 131, (2018/08/04)
Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. (I)
ISOQUINOLINE DERIVATIVES AS MGAT2 INHIBITORS
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Paragraph 0486; 0487, (2018/02/27)
The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia
Hamada, Makoto,Takayama, Tetsuo,Shibata, Tsuyoshi,Hiratate, Akira,Takahashi, Masato,Yashiro, Miyoko,Takayama, Noriko,Okumura-Kitajima, Lisa,Koretsune, Hiroko,Kajiyama, Hiromitsu,Naruse, Takumi,Kato, Sota,Takano, Hiroki,Kakinuma, Hiroyuki
supporting information, p. 1725 - 1730 (2018/04/30)
Prolyl hydroxylase domain-containing protein (PHD) inhibitors are useful as orally administered agents for the treatment of renal anemia. Based on the common structures of known PHD inhibitors, we found novel PHD inhibitor 1 with a 2-[(4-hydroxy-6-oxo-2,3
pyrrole logical sequence handkerchief nai intermediate preparation method (by machine translation)
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Paragraph 0027-0028, (2017/07/06)
The invention relates to a simple operation, raw materials are easy, and the production cost is low, the quality of the product is good and is suitable for the industrial production of the intermediate pyrrole logical sequence handkerchief nai 5 - (pyridine - 2 - yl) - 2 (1H) - pyridone of the preparation method. (by machine translation)
SPIRO-THIAZOLONES
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Page/Page column 76, (2016/06/06)
The present invention provides spiro-thiazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
One-Pot Direct Synthesis of Weinreb Amides from Aryl and Hetero Aryl Halides Using Co 2(CO) 8 as an Effective CO Source under Conventional Thermal Heating
Baburajan, Poongavanam,Elango, Kuppanagounder P.
, p. 541 - 548 (2015/10/29)
A successful protocol for the synthesis of Weinreb amides directly from aryl halides via aminocarbonylation with N,O-dimethyl hydroxylamine using Co2(CO)8 as an in situ CO source has been demonstrated. The effects of various reaction parameters such as temperature, base, and CO source have also been investigated and optimized. GRAPHICAL ABSTRACT.
PARTIALLY SATURATED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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Paragraph 0442; 0443, (2015/06/17)
There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I'): (in the above-mentioned general formula (I'), W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.
HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
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Paragraph 0320; 0321, (2014/05/07)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.