61825-54-5Relevant academic research and scientific papers
(2S)-N-2-methoxy-2-phenylethyl-6,7-benzomorphan compound (2S-LP2): Discovery of a biased mu/delta opioid receptor agonist
Pasquinucci, Lorella,Turnaturi, Rita,Calò, Girolamo,Pappalardo, Francesco,Ferrari, Federica,Russo, Giulia,Arena, Emanuela,Montenegro, Lucia,Chiechio, Santina,Prezzavento, Orazio,Parenti, Carmela
supporting information, p. 189 - 198 (2019/02/27)
The pivotal role of the stereocenter at the N-substituent of the 6,7-benzomorphan scaffold was investigated combining synthetic and pharmacological approaches. 2R- and 2S-diastereoisomers of the multitarget MOR/DOR antinociceptive ligand LP2 (1) were synt
Silylium-Catalyzed Carbon–Carbon Coupling of Alkynylsilanes with (2-Bromo-1-methoxyethyl)arenes: Alternative Approaches
Rubial, Belén,Ballesteros, Alfredo,González, José M.
, p. 6194 - 6198 (2018/07/31)
The catalytic activation of alkynylsilanes towards 2-halo-1-alkoxyalkyl arenes gives β-halo-substituted alkynes. It involves the chemoselective substitution of an alkoxide by an alkyne in the presence of a neighboring C(sp3)–Br bond in a cationic C–C bond-forming event. Two complementary protocols to accomplish this new transformation are reported. The outcome of a direct approach based on mixing the precursors with a freshly prepared solution of the active catalytic species (TMSNTf2) is compared with an alternative based on smooth release of the required silylium ions upon selective activation of the alkyne by gold(I) (JohnPhosAuNTf2). The two approaches gave satisfactory results to access this otherwise elusive alkynylation process, which furnishes 4-bromo-substituted alkynes and tolerates various functional groups.
NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF
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Page/Page column 362, (2014/01/09)
The invention relates to the novel products of formula (I) with p, q = 0, 1 or 2; R1 = phenyl, pyridyl; -(CH2) m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO2 -Rb; -CO-Re; m = 1 or 2; Ra = aryl, heteroaryl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-Rb, -C(Rb)=N-ORc, -CO 2 Rd, -CONRxRy; Rb = alkyl, aryl, heteroaryl; Rc = H, alkyl; Rd = alkyl, cycloalkyl; Re = alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry = H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3 = H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4 = H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
Lewis acid-mediated highly regioselective SN2-type ring-opening of 2-Aryl-N-tosylazetidines and aziridines by alcohols
Ghorai, Manas K.,Das, Kalpataru,Shukla, Dipti
, p. 5859 - 5862 (2008/02/09)
(Chemical Equation Presented) Lewis acid-mediated highly regioselective SN2-type ring-opening of 2-aryl-N-tosylazetidines with alcohols to afford various 1,3-amino ethers in excellent yields with good enantiomeric excess is described. Similar S
