公开(公告)号：US20240140918A1

公开(公告)日：2024-05-02

申请号：US18263513

申请日：2022-01-28

Applicant: TOKYO UNIVERSITY OF SCIENCE FOUNDATION ,  NATIONAL CANCER CENTER

Inventor： Isamu SHIINA ,  Motoyuki SHIMONAKA ,  Takatsugu MURATA ,  Yuuki OBATA ,  Toshirou NISHIDA ,  Koji OKAMOTO

IPC: C07D263/32 ,  C07D213/56 ,  C07D277/30

CPC classification number: C07D263/32 ,  C07D213/56 ,  C07D277/30

Abstract: A compound represented by formula (1) below, useful for treating cancer. In the formula, R1 and R3-R8 each independently represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or a group represented by —ORa, R9 represents a group represented by —C(O)NRcRf, Ra, Re, and Rf each independently represents a hydrogen atom, an arylalkyl group that may have a substituent, or a heteroarylalkyl group. A production method that enables the compound to be produced with high efficiency, and a pharmaceutical composition containing the compound as an active ingredient

公开(公告)号：US20190382425A1

公开(公告)日：2019-12-19

申请号：US15519279

申请日：2015-10-28

Applicant: TOKYO UNIVERSITY OF SCIENCE FOUNDATION

Inventor： Isamu SHIINA ,  Takayuki TONOI

IPC: C07F9/655

Abstract: Provided are: eushearilides; a method for producing eushearilides; a production intermediate; and a pharmaceutical composition containing eushearilides. By having the Wittig reaction process, Mukaiyama Aldol reaction process and Macrolactonizaion process serve as key processes, eushearilides represented by formula (I) are efficiently produced.

公开(公告)号：US20170008820A1

公开(公告)日：2017-01-12

申请号：US15115764

申请日：2015-02-02

Applicant: TOKYO UNIVERSITY OF SCIENCE FOUNDATION

Inventor： Isamu SHIINA

IPC: C07B53/00 ,  C07C269/06 ,  C07D209/48 ,  C07D209/34 ,  C07D209/38 ,  C07B55/00 ,  C07D207/327 ,  C07D209/08 ,  C07D235/06 ,  C07D209/86 ,  C07D207/34 ,  C07D263/58 ,  C07D207/27

CPC classification number: C07B53/00 ,  C07B55/00 ,  C07B2200/07 ,  C07C269/06 ,  C07D207/27 ,  C07D207/327 ,  C07D207/333 ,  C07D207/34 ,  C07D207/416 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D209/38 ,  C07D209/48 ,  C07D209/86 ,  C07D235/06 ,  C07D263/58 ,  C07D403/06 ,  C07D471/04 ,  C07D513/04 ,  C07C271/22

Abstract: Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.

Abstract translation: 提供了一种使用动态动力学拆分制备光学活性羧酸酯的高产率和高对映体选择性的方法，所述光学活性羧酸酯具有α-氮取代基。 该光学活性羧酸酯的制造方法包括使式（a）表示的外消旋羧酸和特定的醇或苯酚衍生物在偶极矩为3.5以下的极性溶剂中，在 酸酐和不对称催化剂，外消旋羧酸的一种对映异构体被选择性酯化，另一种对映体被外消旋化。 在式（a）中，Ra 1表示通过构成环的氮原子键合到比例碳上的含氮杂芳环，Ra2是有机基。