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Enantioselective Synthesis of beta-Aminotetralins via Chiral Phosphoric Acid-catalyzed Reductive Amination of beta-Tetralones
- Park, Do Young;
- Kim, Kyung-Hee;
- Cheon, Cheol-Hong
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18초록
A new protocol for the synthesis of chiral beta-aminotetralins has been developed via chiral phosphoric acid-catalyzed asymmetric reductive amination of beta-tetralones using a Hantzsch ester as an organic hydride donor. Various chiral beta-aminotetralins were obtained in good yields with good to high enantioselectivities. Furthermore, the utility of our new protocol was successfully demonstrated in the enantioselective synthesis of rotigotine.
키워드
beta-Aminotetralins; Asymmetric reductive amination; Chiral phosphoric acid catalysis; Rotigotine; beta-Tetralones; STRONGER BRONSTED ACIDS; IN-VIVO ACTIVITY; PARKINSONS-DISEASE; TRANSFER HYDROGENATION; ASYMMETRIC-SYNTHESIS; RECEPTOR ANTAGONIST; HANTZSCH ESTERS; DOPAMINE; ROTIGOTINE; AGONIST
- 제목
- Enantioselective Synthesis of beta-Aminotetralins via Chiral Phosphoric Acid-catalyzed Reductive Amination of beta-Tetralones
- 저자
- Park, Do Young; Kim, Kyung-Hee; Cheon, Cheol-Hong
- 발행일
- 2018-02-01
- 유형
- Article
- 권
- 360
- 호
- 3
- 페이지
- 462 ~ 467