Takeda Pharmaceutical Company Limited

Hamari Chemicals, Ltd.

Yasuhiko Kawano

Masahiro Kajino

Toshio Miyawaki

Sadayuki Maeda

Tatsunori Sato

Provided are a novel chiral iridium(III) complex; and a method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines from 2-substituted-quinolines with the use of the chiral iridium(III) complex through a more economical and easy production process. The disclosed method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines comprises reducing a quinoline compound represented by formula [I]: in the presence of a hydrogen donor compound and an iridium (III) complex having a chiral prolinamide compound as a ligand to give an optically active 2-substituted-1,2,3,4-tetrahydroquinoline represented by formula [II]: 

Method for producing optically active tetrahydroquinolines

The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Ris a hydrogen atom and the like; Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; Ris unsubstituted (i.e., absence), a hydrogen atom and the like; Rand Rare the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; Ris (cyclic group optionally having substituent(s))-carbonyl, and the like; R, R, Rand Rare the same or different and each is a hydrogen atom, halogen and the like; or Rand R, Rand R, and Rand Rmay form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;--- represents unsubstituted (i.e., absence) or a single bond; andrepresents a single bond or a double bond, or a salt thereof, and the like.

Fused quinoline derivative and use thereof

The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Ris a hydrogen atom and the like; Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; Ris unsubstituted (i.e., absence), a hydrogen atom and the like; Rand Rare the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; Ris (cyclic group optionally having substituent(s))-carbonyl, and the like; R, R, Rand Rare the same or different and each is a hydrogen atom, halogen and the like; or Rand R, Rand R, and Rand Rmay form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;&#x2003;represents unsubstituted (i.e., absence) or a single bond; and&#x2003;represents a single bond or a double bond, or a salt thereof, and the like.

The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Ris a hydrogen atom and the like; Ris a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; Ris unsubstituted (i.e., absence), a hydrogen atom and the like; Rand Rare the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; Ris (cyclic group optionally having substituent(s))-carbonyl, and the like; R, R, Rand Rare the same or different and each is a hydrogen atom, halogen and the like; or Rand R, Rand R, and Rand Rmay form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5;

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Osaka, Japan

Yasuhiko Kawano