Development of a Practical and Scalable Synthesis of a Potent Selective Dual Antagonist for 5-HT2B and 5-HT7 Receptors

Shinya Yoshida; Makoto Kasai; Takenori Kimura

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Development of a Practical and Scalable Synthesis of a Potent Selective Dual Antagonist for 5-HT2B and 5-HT7 Receptors

机译：实用和可扩展合成的5-HT2B和5-HT7受体有效选择性双重拮抗剂的发展。

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Process research and development of a practical and scalable synthetic route toward compound (S)-1 and compound (R)-1, which are potent selective dual antagonists for 5-HT2B and 5-HT7 receptors, respectively, is described. The medicinal chemistry route and second generation route were also unattractive for large-scale use for a variety of reasons. The new synthetic method does not require any purification by column chromatography for all steps and highly exothermic reactions. Additionally, we developed an efficient method of optical resolution in which each carboxylic acid isomer was separated with chiral amine in high yield and high enantiopurity. This highly efficient and scalable process was successfully demonstrated in the large scale synthesis of compound (S)-1 and compound (R)-1 in high enantiopurity.

机译：描述了针对化合物（S）-1和化合物（R）-1的实用且可扩展的合成路线的方法研究和开发，化合物（S）-1和化合物（R）-1分别是针对5-HT2B和5-HT7受体的有效选择性双重拮抗剂。由于多种原因，药物化学路线和第二代路线对于大规模使用也没有吸引力。新的合成方法不需要所有步骤和高度放热反应的柱色谱纯化。此外，我们开发了一种高效的光学拆分方法，其中每个羧酸异构体都可以与手性胺分离，从而获得高收率和高对映体纯度。在高对映体纯度的大规模合成化合物（S）-1和化合物（R）-1中，成功证明了这种高效且可扩展的方法。

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《Organic process research & development》 |2012年第4期|共10页
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Shinya Yoshida; Makoto Kasai; Takenori Kimura;
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1. Development of a Practical and Scalable Synthesis of a Potent Selective Dual Antagonist for 5-HT2B and 5-HT7 Receptors [J] . Shinya Yoshida, Makoto Kasai, Takenori Kimura Organic process research & development . 2012,第4期

机译：实用和可扩展合成的5-HT2B和5-HT7受体有效选择性双重拮抗剂的发展。
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Development of a Practical and Scalable Synthesis of a Potent Selective Dual Antagonist for 5-HT2B and 5-HT7 Receptors

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