title: Preparation of 4-(4'-Hydroxyanilino)-5-anilinophthalimide and 4,5-Bis-(4'-hydroxyanilino)-phthalimide by Microbial Hydroxylation.
abstract: A microbial screening indicated that two fungal strains, Beauveria bassiana DSM 1344=ATCC 7159 and Cunninghamella elegans DSM 1908=ATCC 9245, as well as four bacterial strains belonging to the genus Streptomyces were able to hydroxylate 4,5-dianilinophthalimide (DAPH, CGP52411) to 4-(4'-hydroxyanilino)-5-anilinophthalimide. Cunninghamella elegans DSM 1908 turned out to be the most active biocatalyst and was also able to form the dihydroxy derivative, 4,5-bis(4'-hydroxyanilino)phthalimide. The reaction for the monohydroxylated biotransformation product was carried out on a preparative scale, and the culture conditions for the formation of 4-(4'-hydroxy- anilino)-5-anilinophthalimide with this strain were op-timized.
authors.affiliation: b Institute of Enzyme Technology, Heinrich-Heine-University Düsseldorf, Research Center Jülich.
authors.forename: S
authors.initials: S
authors.lastname: Weidner
authors.affiliation: a Novartis Pharma AG, Research, Core Technology Area, Expertise Bioreactions.
authors.forename: K
authors.initials: K
authors.lastname: Goeke
authors.affiliation: a Novartis Pharma AG, Research, Core Technology Area, Expertise Bioreactions.
authors.forename: U
authors.initials: U
authors.lastname: Trinks
authors.affiliation: c Oncology Research, Novartis Pharma Inc.
authors.forename: P
authors.initials: P
authors.lastname: Traxler
authors.affiliation: a Novartis Pharma AG, Research, Core Technology Area, Expertise Bioreactions.
authors.forename: K
authors.initials: K
authors.lastname: Ucci-Stoll
authors.affiliation: a Novartis Pharma AG, Research, Core Technology Area, Expertise Bioreactions.
authors.forename: O
authors.initials: O
authors.lastname: Ghisalba
keywords: 4,5-bis-(4′-hydroxyanilino)-phthalimide; 4-(4′-hydroxyanilino)-5-anilinophthalimide; PTK-inhibitors; microbial hydroxylation