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Enantioselective synthesis of ferrocenyl nucleoside analogues with apoptosis-inducing activity.
An enantioselective synthesis of novel carbocyclic nucleoside analogues with a ferroceno-cyclopentene backbone was developed and some of the target compounds were shown to exhibit significant apoptosis-inducing activity against tumor cells. Expand
Allylsilanes in Organic Synthesis − Recent Developments
Allylsilanes have been used extensively over the last 30 years. A survey of the most recent advances in this field is described, including transformations of allylsilanes through electrophilic,Expand
Studies on the cytostatic and cytotoxic effects and mode of action of 8-nitro-7-hydroxycoumarin.
A derivative of coumarin, 8-nitro- 7-hydroxycoumarin (8-NO2-7-OHC), was synthesised, purified and characterised and was shown to be non-mutagenic in a standard Ames test, both with or without a mammalian enzyme activation system. Expand
Development of an Efficient Manufacturing Process for Reversible Bruton’s Tyrosine Kinase Inhibitor GDC-0853
Efforts toward the process development of reversible Bruton’s tyrosine kinase (BTK) inhibitor GDC-0853 (1) are described. A practical synthesis of GDC-0853 was accomplished via a key highlyExpand
Free-radical-5-exo-trig cyclization of chiral 3-silylhepta-1,6-dienes: concise approach to the A-B-C ring core of hexacyclinic acid.
Free-radical-mediated 5-exo-trig cyclization of hepta-1,6-dienes 6a-c incorporating an allylsilane moiety was shown to provide at low temperature exclusively the trans-cis cyclopentanes 7a- c in good yield, and Beckwith-Houk-type models were proposed that rationalize the stereochemical course of these 5- Exo-Trig cyclizations. Expand
Radical-mediated 5-exo-trig cyclizations of 3-silylhepta-1,6-dienes.
Thiyl-mediated radical cyclization of dienes 3a, 3c-d, 7 with subsequent sulfur atom transfer was studied, providing thiabicyclo[3.3.0] skeleton in one step with excellent stereocontrol. Expand
Stereoselective Synthesis of New Ferrocene‐Derived Amino Acid Building Blocks
As a contribution to bioorganometallic chemistry, a dia- and enantioselective synthesis of novel carbocyclic amino acid analogues with a 1,2-ferroceno-fused cyclopentene backbone has been developed.Expand
Synthesis and structure-activity relationships of pyrrolidine-modified analogs of the potent cholinergic channel activator, ABT 418
3′ and 5′-substituted pyrrolidine analogs of the potent cholinergic channel activator (ChCA), 3-methyl-5-(2(S)-pyrrolidinyl)-isoxazole (ABT 418), 1, were synthesized and tested in vitro forExpand
Remarkable effect of a silicon group on the stereoselectivity of radical 5-exo-trig cyclizations.
[reaction: see text] Sulfonyl radical mediated 5-exo-trig cyclization of chiral 3-silylhepta-1,6-dienes has been shown to provide cyclopentanes having up to four stereogenic centers with anExpand
Theoretical study of free-radical-mediated 5-exo-trig cyclizations of chiral 3-substituted hepta-1,6-dienes.
Free radical-mediated 5-exo-trig cyclizations of hepta-1,6-dienes incorporating allylsilane, alkyl and alkoxy analogues are modeled using correlated ab initio calculations. The structural, electronicExpand