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. Author manuscript; available in PMC: 2011 Jul 22.
Published in final edited form as: J Med Chem. 2010 Jul 22;53(14):5281–5289. doi: 10.1021/jm100499s

Table 2.

The synthesis of C(3) methylene analogues.

graphic file with name nihms-215550-t0001.jpg

Compound R Yielda
18 graphic file with name nihms-215550-t0002.jpg 80%
19 graphic file with name nihms-215550-t0003.jpg 69%
20 graphic file with name nihms-215550-t0004.jpg 65%
21 graphic file with name nihms-215550-t0005.jpg 90%
22 graphic file with name nihms-215550-t0006.jpg 77%
23 b graphic file with name nihms-215550-t0007.jpg 83%
24 b graphic file with name nihms-215550-t0008.jpg 71%
25 graphic file with name nihms-215550-t0009.jpg 82%

Footnotes:

a

Refers to isolated, purified yields.

b

Used LDA (1.2 equiv) to preform the enolate.