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²Î¿¼ÎÄÏ×£º
1. Org.Proess Res.Dev.2004,8,330-340
2. Journal of the American Chemical Society, 1996, vol. 118, # 9, p. 2301 - 2302
3. J.Org.Chem.2006,71,9045-9050
4. OPRD,2005,9,466-471
5. J.Org.Chem.2005,70-5869-5879
6. Synth.Commum.,1989,19,3139
7. Tetrahedron Letters 45(2004)905-906
8. Journal of Medicinal Chemistry, 2013, vol. 56, # 15, p. 6273 - 6277


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