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US 2014/0228568 A1Published application
Biphenyl derivatives, pharmaceutical composition comprising the same, and preparation method thereof
AssigneeKorea Institute of Science and Technology
InventorsHyunah CHOO, Young-Jae KIm, Jeeyeon KIM, Mi Young YEOM
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Abstract
Provided are biphenyl derivatives exhibiting activity towards central nervous system diseases by acting on the 5-HT7 receptor, pharmaceutically acceptable salts thereof, a method for preparing the compounds and pharmaceutical compositions including the compounds as an active ingredient.
Claims10
A biphenyl derivative represented by the following chemical formula:
- wherein
- each of R1 and R2, which are different, is independently selected from hydrogen, halogen, alkyl, alkoxy, aryloxy and nitro;
- and
- each of R3 and R4, which are different, is independently selected from hydrogen, halogen, alkyl, alkoxy, aryloxy, nitro and phenyl.
1 more element
(canceled)
A method for preparing a biphenyl derivative represented by Chemical Formula 2, comprising:
- preparing a biphenyl aldehyde intermediate represented by Chemical Formula 8 by Suzuki coupling an aryl boronic acid represented by Chemical Formula 6 with bromobenzene aldehyde represented by Chemical Formula 7;
- and
- preparing the compound represented by Chemical Formula 2 by reductive aminating the biphenyl aldehyde intermediate with an arylpiperazine represented by Chemical Formula 9:
- wherein
- each of R1 and R2, which are the same or different, is independently selected from hydrogen, halogen, alkyl, alkoxy, aryloxy and nitro;
- and
- each of R3 and R4, which are the same or different, is independently selected from hydrogen, halogen, alkyl, alkoxy, aryloxy, nitro and phenyl.
4 more elements
Dependencies are inferred from the claim text.