Bicyclo[6.1.0]nonyne carboxylic acid (BCN-COOH) is a valuable intermediate for the development of bioorthogonal click reagents. A convenient three-step synthesis of pure diastereomer -BCN-COOH is reported here, with an overall yield of 32% starting from 1,5-cyclooctadiene. To the best of our knowledge, this is the shortest route to -BCN-COOH known to date. The new method compares favourably with the optimised four-step synthesis based on previously reported data.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11580154 | PMC |
| http://dx.doi.org/10.1039/d4ra06708h | DOI Listing |
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