Process for the preparation of adapalene

Details Process for the preparation of adapalene Process for the preparation of adapalene

2008-03-18

2008-03-18

Eyler, Yvonne (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

C560S100000

Reexamination Certificate

active

11392909

ABSTRACT:
A process for the preparation of a compound of formula (I), or a salt thereofwherein R is H, C1-C8alkyl, aryl or aryl-C1-C8alkyl; comprising the reaction between a compound of formula (II)wherein R1and R2are independently hydrogen, C1-C8alkyl, aryl, aryl-C1-C8alkyl, or R1and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3or C(R3)2wherein R3is hydrogen, C1-C8alkyl, aryl or aryl-C1-C8alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III)in which R4and R5are independently C1-C8alkyl, aryl or aryl-C1-C8alkyl; 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-C8alkyl, aryl or aryl-C1-C8alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

REFERENCES:
patent: 6358541 (2002-03-01), Goodman
Dawson et al., Antagonist Analogue of 6-[3′-(1-Adamantyl)-4′-hydroxyphenyl]-2-naphthalenecarboxylic Acid (AHPN). Family of Apoptosis Inducers That Effectively Blocks AHPN- Induced Apoptosis but Not Cell-Cycle Arrest, J. Med. Chem, 2004, 47, 3518-3536.

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