Kyowa Hakko Bio Co., Ltd.

Dainippon Sumitomo Pharma Co., Ltd.

Sumitomo Dainippon Pharma Co., Ltd.

Tadashi Ogawa

Shinji Kita

Masaji Kasai

Hideaki Tokai

Provided is a process for producing (3R)-2'-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4&#x2032;(1&#x2032;H)-pyrrolo[1,2-a]pyrazine}-1&#x2032;,2,3&#x2032;,5(2&#x2032;H)-tetraone (compound A). The method includes converting an optically active succinimide derivative of formula (I) to compound A, in which the compound of formula (I) has been prepared by reacting a base with an optically active amide derivative of formula (VI).

Process for producing optically active succinimide derivatives and intermediates thereof

A process for producing optically active succinimide derivatives as key intermediates of (3R)-2'-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4&#x2032;(1&#x2032;H)-pyrrolo[1,2-a]pyrazine}-1&#x2032;,2,3&#x2032;,5(2&#x2032;H)-tetraone, which comprises the following reaction steps. 

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Takaoka, Japan

Tadashi Ogawa