Patent · US Expired

Process for the preparation of adapalene

US7345189B2 · kind B2 · utility

0Cited by
1References
13Claims
0Family size

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Key dates

Filing dateMar 30, 2006
Grant dateMar 18, 2008
Priority date
Expiry dateMay 6, 2026

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C2603/74
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A process for the preparation of a compound of formula (I), or a salt thereofwherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II)wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III)in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

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