Japan Tobacco Inc.

Jun-ichi Hoshi

Takahiro Yamasaki

Koji Ando

Koji Matsuda

Shigeji Ohki

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, the present invention provides, for example, compounds represented by the formulas (6), (7-1), (7-2) and (8): wherein R is a fluorine atom or a methoxy group, Ris a C-Calkyl group, Ris a hydroxyl-protecting group, and Xis a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

Process for production of 4-oxoquinoline compound

The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2'): wherein R is a fluorine atom or a methoxy group, and Ris a hydrogen atom or a C-Calkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

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Osaka, Japan

Jun-ichi Hoshi