53750-13-3Relevant articles and documents
Regioselective silver-mediated Kondakov-Darzens olefin acylation
Barczak, Nicholas T.,Jarvo, Elizabeth R.
supporting information; experimental part, p. 12912 - 12916 (2011/12/04)
Enone construction: A silver-mediated olefin acylation reaction is described, in which five-, six-, and -seven-membered rings, tetrasubstituted olefins, bridged bicycles, spirocycles, and benzoxepinones are prepared. Highly selective intermolecular reactions are coupled to a Nazarov cyclization for the effective preparation of cyclopentenones, including the core of modhephene (see scheme). Copyright
Agents for the treatment of overactive detrusor. VII. Synthesis and pharmacological properties of 2,3- and 3,4-diphenylcyclopentylamines, 2,3-diphenyl-2-cyclopentylamines, and related compounds
Taniguchi,Tsubaki,Take,Okumura,Terai,Shiokawa
, p. 896 - 902 (2007/10/02)
As part of our search for new agents for the treatment of overactive detrusor, 2,3- and 3,4-diphenylcyclopentylamines (3), 2,3-diphenyl-2-cyclopentenylamines (4), and related compounds (5 and 18) were synthesized and evaluated for inhibitory activity (i.v.) against urinary bladder rhythmic contraction in rats. Among them, some compounds involving N-tert-butyl-2,3-diphenyl-2-cyclopentenylamine (4b) exhibited inhibitory activity against bladder contraction superior to that of terodiline (2). Mydriatic activity (i.v.) of compound 4b in rats, an index of its side effects due to antimuscarinic activity, was found to be relatively weak in comparison with its inhibitory activity against bladder contraction. The pharmacological profile of 4b was examined in comparisen with that of terodiline. Most of the objective amines (3, 4, 5) were synthesized by preparation of Schiff bases from the corresponding cyclic ketones (6, 7, 8) and amines in the presence of TiCl4 in CH2Cl2 and subsequent reduction with NaBH4 in the presence of MeOH in one pot (method A).
INTRAMOLECULAR ACYLATION OF α-SULFINYL CARBANION: A NEW GENERAL ROUTE TO 5-SUBSTITUTED Δ2-CYCLOPENTENONES
Pohmakotr, Manat,Phinyocheep, Pranee
, p. 2249 - 2252 (2007/10/02)
A general method for the preparation of 5-substituted Δ2-cyclopentenones via the intramolecular acylation of α-sulfinyl carbanions has been demonstrated.