Abstract: An improved process for the preparation of Nabumetone, which comprises the following steps:a) condensation between 6-methoxy-naphthaldehyde I and t-butyl acetoacetate II, to give 3-t-butoxycarbonyl-4-(6'-methoxy-2'-naphthyl)-but-3-en-2-one III as an E/Z mixture;b) hydrogenation of III in the presence of a palladium catalyst, to give 3-t-butoxycarbonyl-4-(6'-methoxy-2-naphthyl)-butan-2-one IV;c) cleavage of the t-butyl ester by acid catalysis; andd) recrystallization of the crude with methanol.
Type:
Grant
Filed:
April 24, 1998
Date of Patent:
September 21, 1999
Assignee:
Secifarma S.P.A.
Inventors:
Walter Cabri, Domenico Magrone, Roberto Angelini, Erminio Oldani
Abstract: A process for the preparation of 3-aminophenylacetylene derivatives of formula: ##STR1## wherein R.sub.1 is as defined in the disclosure ##STR2## wherein Y is as defined in the disclosureR--C.tbd.C--Hwherein R is as defined in the disclosure.
Abstract: An improved process for the resolution of (+)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid into the corresponding enantiomers by using L-threo-(+)-2-amino-1-(4-nitrophenyl)-1,3-propanediol and L-threo-(+)-2-amino-1-(4-methylmercaptophenyl)-1,3-propanediol.
Abstract: The invention relates to a process for the resolution of mixtures of D and L-6-methoxy-alpha-methyl-2-naphthaleneacetic acid in their respective antipodes.L-threo(+)-2-amino-1-p-nitrophenyl-1,3-propandiol is proposed as new resolving agent.