• Journal of the Korean Chemical Society
• /
• v.66 no.1
• /
• pp.9-14
• /
• 2022

An efficient method for the synthesis of 1-aminophthalans has been developed. The intramolecular oxa-Mannich reaction of 1,3-dihydro-2-benzofuran-1-ols with p-toluenesulfonylamine in the presence of Cs₂CO₃ as a base, without using any catalyst, provided the desired 1-aminophthalans in moderate to good yields.

• Bulletin of the Korean Chemical Society
• /
• v.29 no.10
• /
• pp.1946-1950
• /
• 2008

The synthesis of new 5-cyano-1,1-disubstituted phthalans having aromatic and aminoalkyl groups at C-1 position of phthalan ring and their biological evaluation are described. Most compounds exhibited comparable ejaculation-retarding effects to citalopram. Of these compounds, 3a, e showed excellent efficacy in delaying ejaculation.