Eisai R&d Management Co., Ltd.

Harvard College

Isao Ohashi

Keigo Tanaka

Yoshito Kishi

Toshimi Okada

Satoshi Nagao

Kenzo Yahata

Setsuo Funasaka

Takashi Fukuyama

Kentaro Iso

Ning Ye

Qiaoyi Wang

Jihoon Lee

Shuji Yamashita

Santhosh Reddy Naini

Yanran Ai

Yuki Karoji

Yusuke Nakatani

Yoshinobu Yamane

The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A). 

Synthesis of halichondrins

The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or &#x2014;CH&#x2014;; E represents a nitrogen-containing non-aromatic heterocycle; Rrepresents an alkoxy group or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and Ror Ris present on a nitrogen atom on the azetidine ring, the Ror Rdoes not represent a hydrogen atom.

Monocyclic pyridine derivative

Growing community of inventors

Tsukuba, Japan

Isao Ohashi