First Scale-Up Synthesis of WAY-262398, a Novel, Dual-Acting SSRI/5HT1a Antagonist

Antonia Nikitenko; Asaf Alimardanov; Jay Afragola

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First Scale-Up Synthesis of WAY-262398, a Novel, Dual-Acting SSRI/5HT1a Antagonist

机译：新型双向作用SSRI / 5HT1a拮抗剂WAY-262398的首次大规模放大合成

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An alternative synthesis of WAY-262398,1, a novel, dual-acting SSRI/5-HT_(1A) antagonist, has been developed. The target compound was initially synthesized as a part of diastereo-meric mixture which was separated by chiral preparative HPLC. The new route was designed around intermediates suitable for chiral resolution and/or chiral reduction of a suitable intermediate. Both processes had to be employed to achieve the target optical purity.

机译：已开发出一种新型的双作用SSRI / 5-HT_（1A）拮抗剂WAY-262398,1的替代合成物。最初将目标化合物合成为非对映体混合物的一部分，将其通过手性制备型HPLC分离。新路线是围绕适合于手性拆分和/或手性还原合适中间体的中间体设计的。必须采用两种方法才能达到目标光学纯度。

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《Organic process research & development》 |2009年第1期|共7页
作者
Antonia Nikitenko; Asaf Alimardanov; Jay Afragola;
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1. First Scale-Up Synthesis of WAY-262398, a Novel, Dual-Acting SSRI/5HT1a Antagonist [J] . Antonia Nikitenko, Asaf Alimardanov, Jay Afragola Organic process research & development . 2009,第1期

机译：新型双向作用SSRI / 5HT1a拮抗剂WAY-262398的首次大规模放大合成
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First Scale-Up Synthesis of WAY-262398, a Novel, Dual-Acting SSRI/5HT1a Antagonist

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