Agents for the Treatment of Overactive Detrusor. IV. Synthesis and Structure-Activity Relationships of Cyclic Analogues of Terodiline.

Multifunctional Nitrogen‐Doped Carbon Nanodots for Photoluminescence, Sensor, and Visible‐Light‐Induced H2 Production

“…18c: Known compound; the 1 H NMR spectroscopic data agree with those given in ref 52 . 1 H NMR (CDCl 3 , 400 MHz): δ =4.08 (s, 2 H), 4.53 (s, 2 H), 6.95–7.00 (m, 3 H), 7.32–7.39 (m, 7 H); 13 C NMR (CDCl 3 , 100.6 MHz): δ =39.7, 55.9, 115.8, 115.9, 120.8, 127.8, 128.0, 129.0, 129.7, 136.9, 148.1; IR (neat/ATR probe): ν =3062, 3029, 2925, 2852, 1598, 1579, 1503, 1495, 1452, 1426, 1357, 1221, 1199, 1168, 1027, 960, 937, 869, 749, 729, 690 cm −1 ; HR‐MS (EI): m/z =222.1156, calcd.…”

Synthesis and Anticholinergic Activity of the Four Stereoisomers of 4-(Dimethylamino)-2-phenyl-2-(2-pyridyl)pentanamide

“…Greater activity was seen with both racemates 8 and 9 in comparison with compound 3, suggesting that the introduction of a methyl group affected an increase of activity. Regarding the stereochemistry at the 2-and 4-positions, the 2S,4fi-isomer (13) exhibited the most potent activity. The 2R,4fi-isomer (10) was shown to be the second strongest, albeit with 3 times less activity.…”

“…(-)-(2S,4JZ)-4-(Dimethylamino)-2-phenyl-2-(2-pyridyl)pentanamide (13). The filtrate, which was obtained in the isolation of 12, was concentrated under reduced pressure.…”

“…The corresponding (+)-enantiomer 11 was isolated from the mother liquor as a salt of (+)-dibenzolyl-D-tartaric acid. Recrystallization of the (-)-dibenzoyl-L-tartrate of 9 afforded (+)-enantiomer 12 as a crystalline salt, while (-)-enantiomer 13 was obtained from the mother liquor. The enantiomeric purities of these compounds were assessed by HPLC analyses using a chiral column and were >99% ee.…”

Domino Synthesis of 4‐Alkylidene‐3,4‐dihydro‐2H‐pyrroles from Homopropargyl Sulfonamides and Aldehydes

“…These compounds have been synthesized by intramolecular aza‐Wittig reactions of α ‐azidoethyl‐ α , β ‐enones using Ph 3 P, [1a,2a,b] by cyclization reactions of nitrilium ions (nitrilium cyclization) derived from homoallyl carboxamides, [2c,3a] by metathesis reactions of alkynyl Fischer carbene complexes with imines [2d] and by condensation reactions of dihydropyrroles with aldehydes [1b,4] . As the alternative methods, the cyclization of other acyclic precursors, [3] nitrilium cyclization of 1,3‐diols [5a,b] or vinylidenecyclopropanes [5c] with nitriles, and miscellaneous methods [6] have been known. However, these procedures are met with the use of highly explosive substrates, the use of a large excess amount of substrates or acids, multi‐step synthesis process of substrates, the use of expensive catalysts and/or substrate limitations.…”