1192-08-1Relevant academic research and scientific papers
Round-Trip Radical Probes: Ring Cleavage of the Bicyclopentylcarbinyl Radical
Branchaud, Bruce P.,Glenn, Anne G.,Stiasny, Hans C.
, p. 6656 - 6659 (1991)
The novel concept of a round-trip probe for radical intermediates in reaction mechanisms is proposed and defined in this paper.A round-trip radical probe undergoes skeletal rearrangements such that the radical is returned to its site of origin.These probes should be especially useful for the study of enzyme mechanisms, since the special requirements of the active site may lead to ambiguous results using standard nonround-trip radical probes.The ring cleavages and rearrangements of the bicyclopentylcarbinyl radical are described as the prototypical round-trip radical probe.We have measured the rate constant for the ring opening of the bicyclopentylcarbinyl radical over the temperature range -42 to 60 deg C and have determined a temperature-dependent function for the ring opening of log (k3/s-1) = 12.78 (+/-0.26) - 7.79 (+/-0.35)/θ and a rate constant for ring opening of 1.15 * 107 s-1 at 25 deg C.
HPK1 INHIBITORS, PREPARATION METHOD AND APPLICATION THEREOF
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Page/Page column 153; 154, (2019/11/12)
Disclosed are HPK-1 inhibitors having a structure represented by Formula (X), pharmaceutical compositions comprising the HPK-1 inhibitors, methods of using the HPK-1 inhibitors, such as treating cancers, methods of preparing the HPK-1 inhibitors, and the synthetic intermediates.
Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer's disease
Monenschein, Holger,Horne, Daniel B.,Bartberger, Michael D.,Hitchcock, Stephen A.,Nguyen, Thomas T.,Patel, Vinod F.,Pennington, Lewis D.,Zhong, Wenge
scheme or table, p. 3607 - 3611 (2012/07/17)
The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off target toxicity, and improved micr
BETA-SECRETASE MODULATORS AND METHODS OF USE
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Page/Page column 161, (2010/11/27)
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.
Vinyl Cations, 38. Synthesis and Solvolysis of 3-Substituted 1-Cyclobutenyl Nonaflates
Auchter, Gerhard,Hanack, Michael
, p. 3402 - 3413 (2007/10/02)
3-Methyl- (8a) and 3-cyclopropyl-1-cyclobutenyl nonaflate (8b) as well as 2-cyclopropyl-1-cyclobutenyl nonaflate (12) and the parent 1-cyclobutenyl nonaflate (3) were synthesized from the corresponding cyclobutanones and nonafluorobutanesulfonic anhydride (10).The solvolysis rates and the product compositions of the solvolyses in trifluoroethanol and trifluoroethanol/water mixtures were determined.All 1-cyclobutenyl nonaflates solvolyze via a SN1 mechanism involving the intermediate nonclassical 1-cyclobutenyl cation, which is additionally stabilized by the substituents in the 3-position.
