Eisai R&d Management Co., Ltd.

Banyu Pharmaceutical Co. Ltd

Atsushi Akao

Taiju Nakamura

Hirofumi Kuroda

Taichi Abe

Yusuke Ayata

Yusuke Miyashita

Toshiaki Mase

Masashi Kawasaki

Fumio Nakano

Takahiro Itoh

Shouichi Hiraga

Asayuki Kamatani

Masayuki Hagiwara

Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less. 

High-purity quinoline derivative and method for manufacturing same

Disclosed is an efficient and widely-applicable method for commercially producing a thioether compound or a thiol compound which is useful as a pharmaceutical compound or a production intermediate of it. Specifically disclosed is a method for producing a thioether compound represented by the general formula [I] below or a salt thereof. This method is characterized in that a compound represented by the following general formula [III]: [III] (wherein X represents a bromine atom, a chlorine atom or a trifluoromethylsulfonyloxy group, and ring A represents an aryl group or a heteroaryl ring group) or a salt thereof is reacted with a thiol compound represented by the following general formula [II]: [II] or a salt thereof in the presence of a palladium compound such as Pd(dba), a base such as i-PrNEt and a phosphorus compound represented by the following formula [AA].

Method for producing thioether compound

A process for preparing indolopyrrolocarbazole derivatives &lsqb;I&rsqb; by trating a compound &lsqb;V&rsqb; with a base in an inert solvent to prepare a compound &lsqb;IV&rsqb;, reacting the compound &lsqb;IV&rsqb; with a compound &lsqb;III&rsqb;to prepare a compound &lsqb;II&rsqb;, and deblocking the compound &lsqb;II&rsqb;; intermediates &lsqb;II&rsqb;, &lsqb;III&rsqb; and &lsqb;IV&rsqb;; and a process for preparing compounds &lsqb;III&rsqb;: &lsqb;wherein Y is hydrogen, C alkyl, phenyl, benzyloxymethyl, or aralkyl; R , R , R , R , R , and R are each independently a hydroxyl-protecting group; R and R are each independently hydrogen or a hydroxyl-protecting group; and X is an acid molecule&rsqb;. The above process is a safe and easy industrial process for preparing indolopyrrolocarbazole derivatives &lsqb;1&rsqb; useful as antitumor agents.

Process for preparing indolopyrrolocarbazole derivatives, intermediates therefor, and preparation process of the intermediates

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Kamisu, Japan

Atsushi Akao