A new efficient and concise enantioselective synthetic method for (−)-horsfiline is reported. (−)-Horsfiline could be obtained from diphenylmethyl tert-butyl malonate in 9 steps (32 %,>99 % ee) by using the enantioselective phase-transfer catalytic allylation (91 % ee) as the key step. This approach can be applied as a practical route for the large-scale synthesis of spirooxindole natural products, which enables a systematic investigation of their biological activity to be performed.
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