An efficient synthesis of a heterobifunctional coupling agent |
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Authors: | Reddy Rajarathnam E Chen Yon-Yih Johnson Donald D Beligere Gangamani S Rege Sushil D Pan You Thottathil John K |
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Institution: | Core R&D Chemistry Group (Department 09MD, Building AP20), Diagnostics Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6016, USA. rajarathnam.reddy@abbott.com |
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Abstract: | An efficient synthesis of 4-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)methyl]-N-(6-6-(6-(2,5-dioxopyrrolidin-1-yl)oxy]-6-oxohexyl]amino)-6-oxohexyl]amino]-6-oxohexyl)cyclohexanecarboxamide (12), a heterobifunctional coupling agent, was developed, which is critical for chemoselective conjugation of proteins and enzymes. The synthesis involved seven steps starting from 6-{(benzyloxy)carbonyl]amino}hexanoic acid (1), and multigram quantities of coupling agent (12) were prepared using this protocol in excellent overall yield and 99.6% purity by reversed phase HPLC. The new method is suitable for the synthesis of coupling agent 12, consistently with purity >99%, and is useful for the preparation of other analogous coupling agents. |
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