公开(公告)号：US20130310595A1

公开(公告)日：2013-11-21

申请号：US13684126

申请日：2012-11-21

Applicant: Japan Tobacco Inc.

Inventor： Koji MATSUDA ,  Koji ANDO ,  Shigeji OHKI ,  Jun-ichi HOSHI ,  Takahiro YAMASAKI

IPC: C07C69/716 ,  C07C57/76 ,  C07C57/72 ,  C07C69/708

CPC classification number: C07C229/30 ,  C07C43/215 ,  C07C57/72 ,  C07C57/76 ,  C07C61/40 ,  C07C67/333 ,  C07C67/343 ,  C07C69/708 ,  C07C69/716 ,  C07C69/738 ,  C07C69/92 ,  C07C69/94 ,  C07C229/34 ,  C07D215/56

Abstract: 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 R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

Abstract translation: 本发明提供了可用作具有整合酶抑制活性的抗HIV剂的合成中间体的化合物及其制备方法，以及使用该合成中间体的抗HIV剂的制备方法。 具体而言，例如，式（2'）表示的化合物或其盐，其中R为氟原子或甲氧基，R400为氢原子或C1-C4烷基， 以及使用该合成中间体的抗HIV剂的制造方法。

公开(公告)号：US20180265454A1

公开(公告)日：2018-09-20

申请号：US15789779

申请日：2017-10-20

Applicant: Japan Tobacco Inc.

Inventor： Koji MATSUDA ,  Koji ANDO ,  Shigeji OHKI ,  Jun-ichi HOSHI ,  Takahiro YAMASAKI

IPC: C07C229/30 ,  C07C57/72 ,  C07C61/40 ,  C07C69/738 ,  C07D215/56 ,  C07C67/343 ,  C07C67/333 ,  C07C57/76 ,  C07C69/716 ,  C07C69/92 ,  C07C69/94 ,  C07C43/215 ,  C07C69/708 ,  C07C229/34

CPC classification number: C07C229/30 ,  C07C43/215 ,  C07C57/72 ,  C07C57/76 ,  C07C61/40 ,  C07C67/333 ,  C07C67/343 ,  C07C69/708 ,  C07C69/716 ,  C07C69/738 ,  C07C69/92 ,  C07C69/94 ,  C07C229/34 ,  C07D215/56

Abstract: 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 R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

公开(公告)号：US20130345462A1

公开(公告)日：2013-12-26

申请号：US13741214

申请日：2013-01-14

Applicant: JAPAN TOBACCO INC.

Inventor： Koji MATSUDA ,  Koji ANDO ,  Shigeji OHKI ,  Takahiro YAMASAKI ,  Jun-ichi HOSHI

IPC: C07C229/30 ,  C07C65/21 ,  C07F7/18

CPC classification number: C07C229/30 ,  C07C65/21 ,  C07C69/716 ,  C07C229/34 ,  C07D215/233 ,  C07D215/56 ,  C07F7/1804 ,  Y02P20/55

Abstract: 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, R1 is a C1-C4 alkyl group, R2 is a hydroxyl-protecting group, and X2 is a halogen atom, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.