- Nitrile Synthesis by Aerobic Oxidation of Primary Amines and in situ Generated Imines from Aldehydes and Ammonium Salt with Grubbs Catalyst
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Herein, a Grubbs-catalyzed route for the synthesis of nitriles via the aerobic oxidation of primary amines is reported. This reaction accommodates a variety of substrates, including simple primary amines, sterically hindered β,β-disubstituted amines, allylamine, benzylamines, and α-amino esters. Reaction compatibility with various functionalities is also noted, particularly with alkenes, alkynes, halogens, esters, silyl ethers, and free hydroxyl groups. The nitriles were also synthesized via the oxidation of imines generated from aldehydes and NH4OAc in situ. (Figure presented.).
- Utsumi, Tatsuki,Noda, Kenta,Kawauchi, Daichi,Ueda, Hirofumi,Tokuyama, Hidetoshi
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p. 3583 - 3588
(2020/08/05)
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- COMPOSITIONS FOR PROMOTING READTHROUGH OF PREMATURE TERMINATION CODONS, AND METHODS OF USING THE SAME
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Disclosed are compounds of general formula (I) that promote readthrough of a premature termination codon (PTC) of an RNA molecule in a translation system, and their use, alone or in combination with other compounds, such as aminoglycoside, to treat diseases or disorders ameliorated by modulation of a premature termination codon (PTC) of an RNA molecule in a translation system. The disorder or disease may be Dystrophic epidermolysis bullosa, Batten disease, Duchenne muscular dystrophy, cancer, and spinal muscular atrophy. Ar-L-B (I)
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Page/Page column 214; 216; 217; 224
(2017/04/11)
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- Synthesis and cross-coupling reactions of imidomethyltrifluoroborates with aryl chlorides
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Potassium imidomethyltrifluoroborate salts were efficiently synthesized. Potassium phthalimidomethyltrifluoroborate was successfully used in Suzuki-Miyaura-like cross-coupling reactions with a variety of aryl chlorides.
- Devulapally, Rammohan,Fleury-Brégeot, Nicolas,Molander, Gary A.,Seapy, Dave G.
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supporting information; experimental part
p. 1051 - 1055
(2012/03/26)
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- Di-μ-hydroxy-bis(N,N,N′,N′-tetramethylenediamine)-copper(II) chloride [Cu(OH)·TMEDA]2Cl2: An efficient, practical catalyst for benzylation and allylation of amides
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An efficient protocol for the benzylation or allylation of amides using the corresponding benzyl or allyl chlorides as electrophiles under basic conditions with commercially available 5 mol % of [Cu(OH)TMEDA]2Cl2 as catalyst was developed. Under these conditions, unprotected amino acids were benzylated without any racemization.
- Kumaraswamy,Pitchaiah,Ramakrishna,Ramakrishna,Sadaiah
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p. 2013 - 2015
(2007/10/03)
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- Access to the new isoindolo[1,3]benzothiazocinones via the combination of N-acyliminium chemistry and friedel-crafts type π-cyclization
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New racemic and chiral [4,2]- and [3,5]benzothiazocines (4) and (5) in the isoindolinone series were synthesized easily in few steps based on the combination of N-acyliminium chemistry and π-cationic cyclization of acylium ions. The chemoselectivity observed during these processes, particularly in the reduction, the thioalkylation and the cyclization stages, were also discussed.
- Cul, Armelle,Daich, Adam,Decroix, Bernard,Sanz, Gerard,Van Hijfte, Luc
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- Prostanoids and related compounds. VII. Synthesis and inhibitory activity of 1-isoindolinone derivatives possessing inhibitory activity against thromboxane A2 analog (U-46619)-induced vasoconstriction
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We have synthesized a series of novel 1-isoindolinone derivatives, which inhibited the contraction of pig coronary artery induced by U-46619, a thromboxane A2 analog.
- Kato, Yoshiaki,Takemoto, Masumi,Achiwa, Kazuo
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p. 529 - 535
(2007/10/03)
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- Benzylphthalimides and phenethylphthalimides with thalidomide-like activity on the production of tumor necrosis factor α
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Benzylphthalimide analogs (P1P's) and phenethylphthalimide analogs (P2P's) have been found to exhibit thalidomide-like activity on the production of tumor necrosis factor (TNF)-α by the human leukemia cell line, HL-60, stimulated by 12-O-tetradecanoylphorbol-13-acetate (TPA). Structure-activity relationships are discussed on the basis of the TNF-α production-enhancing activity. Benzylphthalimide (P1P-00) exhibited activity which is weaker than that of thalidomide, but introduction of a methyl group at the ortho-position of the benzyl moiety (P1P-10) resulted an increase to a level comparable with that of thalidomide. Phenethylphthalimide (P2P-00) is more potent than thalidomide, and its fluorinated derivative, 2-phenethyl-4,5,6,7-tetrafluoro- 1H-isoindole-1,3-dione (FP2P-00), exhibited potent activity at very low concentrations.
- Sasaki,Shibata,Hashimoto,Iwasaki
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p. 1228 - 1233
(2007/10/03)
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