Pilot-Plant Preparation of an α_vβ3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling

Gerald A. Weisenburger; D. Keith Anderson; Jerry D. Clark

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Pilot-Plant Preparation of an α_vβ3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling

机译：α_vβ3整合素拮抗剂的中试制备：羰基二咪唑肽偶联剂的工艺开发

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The process development of a peptide coupling with CDI is discussed. Various solvents, addition orders, stoichiometrics, and reaction temperatures were investigated. A reliable crystallization procedure was also developed. The new process was piloted to provide 342 kg of product in two batches with an average 85% yield and 99% assay.

机译：讨论了与CDI偶联的肽的工艺开发。研究了各种溶剂，添加顺序，化学计量和反应温度。还开发了可靠的结晶程序。新工艺进行了试生产，分两批提供342千克产品，平均收率达85％，化验率为99％。

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《Organic process research & development》 |2009年第1期|共4页
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Gerald A. Weisenburger; D. Keith Anderson; Jerry D. Clark;
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1. Pilot-Plant Preparation of an α_vβ3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling [J] . Gerald A. Weisenburger, D. Keith Anderson, Jerry D. Clark Organic process research & development . 2009,第1期

机译：α_vβ3整合素拮抗剂的中试制备：羰基二咪唑肽偶联剂的工艺开发
2. Pilot-plant preparation of an alpha(v)beta(3) integrin antagonist. Part 2. Synthesis of N-[2-(5-hydroxy-4,6-tetrahydropyrimidine)]-3-amino-5-hydroxybenzoic acid [J] . Clark JD, Collins JT, Kleine HP, Organic process research & development . 2004,第4期

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Pilot-Plant Preparation of an α_vβ3 Integrin Antagonist: Process Development of a Carbonyldiimidazole Peptide Coupling

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