Process for the preparation of adapalene

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United States of America Patent

PATENT NO 7345189
APP PUB NO 20060229465A1
SERIAL NO

11392909

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A process for the preparation of a compound of formula (I), or a salt thereof ##STR00001## wherein R is H, C.sub.1-C.sub.8 alkyl, aryl or aryl-C.sub.1-C.sub.8 alkyl; comprising the reaction between a compound of formula (II) ##STR00002## wherein R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-C.sub.8 alkyl, aryl, aryl-C.sub.1-C.sub.8 alkyl, or R.sub.1 and R.sub.2, taken together, form a --(CH.sub.2).sub.m--V--(CH.sub.2).sub.n-- group, in which V is NR.sub.3 or C(R.sub.3).sub.2 wherein R.sub.3 is hydrogen, C.sub.1-C.sub.8 alkyl, aryl or aryl-C.sub.1-C.sub.8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) ##STR00003## in which R.sub.4 and R.sub.5 are independently C.sub.1-C.sub.8 alkyl, aryl or aryl-C.sub.1-C.sub.8 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 C.sub.1-C.sub.8 alkyl, aryl or aryl-C.sub.1-C.sub.8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

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Patent Owner(s)

Patent OwnerAddress
LUNDBECK PHARMACEUTICALS ITALY S P AITALY PADOVA PADUA PADUA

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Allegrini, Pietro San Donato Milanese, IT 114 341
Castaldi, Graziano Briona, IT 87 309
Ercoli, Mauro Milan, IT 4 0
Razzetti, Gabriele Sesto S. Giovanni, IT 65 118

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