Patent · US Active

Process for the preparation of 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole and the hydrogensulfate salt thereof

US11352346B2 · kind B2 · utility

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Key dates

Filing dateNov 30, 2018
Grant dateJun 7, 2022
Priority date—
Expiry dateNov 30, 2038

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07F7/10
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present disclosure relates to an improved process for the preparation of isochroman structured alpha2A adrenoceptor agonist, namely 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole of formula (I) and a pharmaceutically acceptable salts thereof, such as 2-(5-methoxyisochroman-1-yl)-4,5-dihydro-1H-imidazole hydrogensulfate of formula (Ia), and to a novel intermediate compound used in the process, namely N-(2-aminoethyl)-5-methoxyisochroman-1-carboxamide monohydrate of formula (V). Alpha2A agonists are useful in the treatment of anxiety, and for use as a sedative or analgesic agent, and other diseases where alpha2A agonism is desired.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.