The synthesis of 3-aryl-3-azetidinyl acetic acid esters by rhodium(I)-catalysed conjugate addition of organoboron reagents |
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| Authors: | Philip N Collier |
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| Institution: | Vertex Pharmaceuticals (Europe) Ltd., 88 Milton Park, Abingdon, Oxfordshire OX14 4RY, UK |
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| Abstract: | A practical route to 3-aryl-3-azetidinyl acetic acid esters is developed. The key step involves the rhodium(I)-catalysed conjugate addition of an organoboron reagent to an α,β-unsaturated alkene. Elaboration of one conjugate addition product to give a novel spiroazetidine ring system is also described. |
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