Agents for the treatment of overactive detrusor. V. Synthesis and inhibitory activity on detrusor contraction of N-tert-butyl-4, 4-diphenyl-2-cyclopentenylamine.

…, K OKUMURA, K TSUBAKI, K TANIGUCHI…

文献索引：Take, Kazuhiko; Okumura, Kazuo; Tsubaki, Kazunori; Taniguchi, Kiyoshi; Terai, Takao; Shiokawa, Youichi Chemical and Pharmaceutical Bulletin, 1996 , vol. 44, # 10 p. 1858 - 1864

全文：HTML全文

被引用次数: 8

摘要

N-tert-Butyl-4, 4-diphenyl-2-cyclopentenylamine ((±)-3) was designed to restrict the conformation of terodiline 1 and was synthesized in a 6-step approach starting with diphenylacetaldehyde (10) or in a 4-step approach starting with 2, 2-diphenyl-4-pentenoic acid (17). Using di-p-toluoyltartaric acid as a resolving agent, the synthetic (±)-3 was resolved into its optically pure forms,(-)-and (+)-3. The (-)-enantiomer (-)-3· HCl (FK584) ...