60737-65-7Relevant academic research and scientific papers
Photochemical Deracemization of Allenes and Subsequent Chirality Transfer
Bach, Thorsten,Jandl, Christian,Plaza, Manuel
, p. 12785 - 12788 (2020)
Trisubstituted allenes with a 3-(1′-alkenylidene)-pyrrolidin-2-one motif were successfully deracemized (13 examples, 86–98 percent ee) employing visible light (λ=420 nm) and a chiral triplet sensitizer as the catalyst (2.5 mol percent). The photocatalyst
Synthesis of Lactams by Reductive Amination of Carbonyl Derivatives with ω-Amino Fatty Acids under Hydrosilylation Conditions
Tongdee, Satawat,Wei, Duo,Wu, Jiajun,Netkaew, Chakkrit,Darcel, Christophe
supporting information, p. 5536 - 5539 (2021/08/07)
An efficient method for the preparation of lactams from ω-amino fatty acids under hydrosilylation is described. A variety of lactams such as pyrrolidinones, piperidinones and 2-azepanones were selectively synthesised in moderate to excellent yields (29 examples, up to 95 % isolated yields) with a good functional group tolerance. Notably, no metallic based catalyst was required to perform this transformation.
Facile Synthesis of Spirocyclic Lactams via [3+2] and [3+3] Aza-Annulation Reactions
Hayrapetyan, Davit,Stepanova, Valeriya
supporting information, p. 2121 - 2125 (2021/07/26)
Spirocyclic pyrrolidones and piperidones were synthesized starting from readily available α-ketolactones and α-ketolactams employing [3+2]- and [3+3]-aza-annulation reactions. Annulation reactions proceeded with good yields and further reduction of the ex
CHEMICAL COMPOUNDS
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Page/Page column 137, (2020/06/01)
A compound of formula (I), wherein Ar1, R21, R23, R24, R25, R26, R27, A, X, Y and W are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
PHARMACEUTICALLY EFFECTIVE COMPOUNDS INHIBITING SELECTIVELY THE MYOSIN 2 ISOFORMS
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, (2019/11/12)
The present invention relates to compounds of formula (I) or (II) (I) (II) pharmaceutically acceptable salts, solvates, tautomers, stereoisomers thereof, including enantiomers, diastereomers, racemic mixtures, mixtures of enantiomers, or combinations ther
Transition-Metal-Free Deconstructive Lactamization of Piperidines
Romero-Iba?ez, Julio,Cruz-Gregorio, Silvano,Sandoval-Lira, Jacinto,Hernández-Pérez, Julio M.,Quintero, Leticia,Sartillo-Piscil, Fernando
supporting information, p. 8867 - 8871 (2019/05/28)
One of the major challenges in organic synthesis is the activation or deconstructive functionalization of unreactive C(sp3)–C(sp3) bonds, which requires using transition or precious metal catalysts. We present here an alternative: the deconstructive lactamization of piperidines without using transition metal catalysts. To this end, we use 3-alkoxyamino-2-piperidones, which were prepared from piperidines through a dual C(sp3)–H oxidation, as transitory intermediates. Experimental and theoretical studies confirm that this unprecedented lactamization occurs in a tandem manner involving an oxidative deamination of 3-alkoxyamino-2-piperidones to 3-keto-2-piperidones, followed by a regioselective Baeyer–Villiger oxidation to give N-carboxyanhydride intermediates, which finally undergo a spontaneous and concerted decarboxylative intramolecular translactamization.
The first synthesis and antioxidant and anticholinergic activities of 1-(4,5-dihydroxybenzyl)pyrrolidin-2-one derivative bromophenols including natural products
Rezai, Mohsen,Bayrak, ?etin,Taslimi, Parham,Gül?in, Ilhami,Menzek, Abdullah
, p. 808 - 825 (2018/06/07)
We report herein the first synthesis of biologically active natural bromophenols, namely 1-(2,3,6-tribromo-4,5-dihydroxybenzyl)pyrrolidin-2-one (2), 2RS-1-(2,3-dibromo-4,5-dihydroxybenzyl)-5-oxopyrrolidine-2-carboxylic acid (3), and 2RS-methyl 1-(2,3-dibr
COMPOUNDS, COMPOSITIONS, AND METHODS
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Paragraph 0182; 0213, (2017/09/27)
The present disclosure relates generally to compounds of formula (I) or a pharmaceutically acceptable salt, prodrug, deuterated analog, tautomer, stereoisomer, or mixture of stereoisomers thereof and their use as LRRK2 inhibitors.
Iridium-Catalyzed Single-Step N-Substituted Lactam Synthesis from Lactones and Amines
Kim, Kicheol,Hong, Soon Hyeok
, p. 4152 - 4156 (2015/05/04)
Catalytic lactam synthesis was achieved directly from lactones and amines using an Ir catalyst. Three sequential transformations - aminolysis of lactone, N-alkylation of amine with hydroxyamide, and intramolecular transamidation of aminoamide - afforded the corresponding N-substituted lactams. (Figure Presented).
HETEROCYCLIC COMPOUND
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Paragraph 0369, (2015/03/03)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
