期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 6, 期 24, 页码 4567-4574出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/b812777h
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资金
- DFG [Ro985/21]
The present report is concerned with a stereoselective, reliable route to trans-1,2-disubstitutedcyclopropanes and in particular to (S,S)-1-tosyloxymethyl-2-fluoromethyl-cyclopropane (1) and (R,R)-1-tosyloxymethyl-2-fluoromethyl-cyclopropane (ent-1) as conformationally restricted, terminally fluorinated C-4-building blocks for medicinal chemistry. The enzymatic kinetic resolution based synthesis of 1 and ent-1 utilises inexpensive, commercially available starting materials. It is based on enantiomeric resolution of rac-cyclopropane carboxylic esters using esterase from Streptomyces diastatochromogenes. Both enantiomers of 1 were prepared selectively in high overall yield over nine steps, starting from ethyl acrylate. The successful radiosynthesis of [F-18]-1 and [F-18]-ent-1 is also reported.
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