Efficient and practical in situ zinc activation was accomplished by treatment with catalytic amount of an organic acid. The protocol was applied successfully to the Blaise reaction of various nitriles. Noteworthy is the excellent Blaise transformation of (S)-4-chloro-3-trimethylsilyloxybutyronitrile (2b) into tert-butyl (S)-6-chloro-5-hydroxy-3-oxohexanoate (1), a key intermediate for the preparation of HMG-CoA reductase inhibitors (statins).
Other bioactive products U 1300Gamnamoside, a Phenylpropanoid Glycoside from Persimmon Leaves (Diospyros kaki) with an Inhibitory Effect Against an Alcohol Metabolizing Enzyme. -From the aqueous methanol extract of the title leaves, gamnamoside (I) is isolated together with osmanthuside and (-)-catechin. All compounds show good inhibitory activity against alcohol dehydrogenase. -(VARUGHESE, T.; RAHAMAN, M.; KIM, N.
Efficient synthesis of clitocine has been accomplished via unprecedented 1,3-N (endo) to N (exo) migration as a key transformation. Incorporation of p-chlorobenzoyl (PCB) group as a protecting group led to the easy solidification of the intermediate of 7, thus making the isolation very facile and to the minimization of the epimerization of the anomeric center at the final deprotection stage.
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