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Abstract The Pd‐catalyzed carbon‐carbon bond formation pioneered by Heck in 1969 has dominated medicinal chemistry development for the ensuing fifty years. As the demand for more complex three‐dimensional active pharmaceuticals continues to increase, preparative enzyme‐mediated assembly, by virtue of its exquisite selectivity and sustainable nature, is poised to provide a practical and affordable alternative for accessing such compounds. In this minireview, we summarize recent state‐of‐the‐art developments in practical enzyme‐mediated assembly of carbocycles. When appropriate, background information on the enzymatic transformation is provided and challenges and/or limitations are also highlighted.more » « less
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