title: Synthetic study on the unique dimeric arylpiperazine: access to the minor contaminant of aripiprazole.
abstract: The dimeric derivative of aripiprazole was synthesized via the two notable synthetic technologies as a key step: (1) efficient aldehyde bis-arylation by Bi(OTf)(3) and (2) facile Wynberg amination at room temperature. The synthesis has established the structural identity with the minor contaminant sometimes present in Aripiprazole.
authors.affiliation: Process Research Laboratory, Second Tokushima Factory, Otsuka Pharmaceutical Co., Ltd., Kawauchi-cho, Japan. torisawa@fact.otsuka.co.jp
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Torisawa
authors.forename: Koichi
authors.initials: K
authors.lastname: Shinhama
authors.forename: Takao
authors.initials: T
authors.lastname: Nishi
authors.forename: Jun-ichi
authors.initials: J
authors.lastname: Minamikawa
mesh_terms: D000586:Amination; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000737:chemistry; D000068180:Aripiprazole; D019281:Dimerization; D004340:Drug Contamination; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D014150:Antipsychotic Agents; D010879:Piperazines; D015363:Quinolones; D000068180:Aripiprazole