Diastereoselective α-alkylation of 2-acyl-3-phenyl-l-menthopyrazoles
N-Acylpyrazoles were α-alkylated in good yields by the treatment with alkyl halides after metalation with LDA or LiHMDS. In the case of chiral N-acylpyrazoles, e.g., 2-acyl-3-phenyl-l-menthopyrazoles (4), the α-alkylation was highly diastereoselective. The subsequent α-alkylation products could be converted into esters in good yield in the presence of BF3·OEt2 without the loss of the optical purity.
Kashima,Fukuchi,Hosomi
p. 7821 - 7824
(2007/10/02)
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