- MACROCYCLIC SPIROETHERS AS MCL-1 INHIBITORS
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Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.
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Paragraph 0535; 0536
(2020/07/31)
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- Synthesis of a C1-C11 fragment of Zincophorin using planar chiral, neutral π-allyl iron complexes
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A key step in the synthesis of a C1-C11 fragment of the ionophore antibiotic Zincophorin involves the addition of an α-alkoxyalkylcopper(i) reagent to a planar chiral, neutral π-allyl iron complex. The key allylic alkylation reaction is highly regio- and
- Cooksey, John P.
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p. 5117 - 5126
(2013/08/23)
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- Progress toward the total synthesis of callipeltin A (I): Asymmetric synthesis of (3S,4R)-3,4-dimethylglutamine
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(equation presented) During the total synthesis of the novel cyclic depsipeptide callipeltin A (1), the unit (3S,4R)-3,4-dimethylglutamine, was successfully synthesized by asymmetric Michael addition and subsequent electrophilic azidation. The key feature of this approach is the generation of three adjacent stereogenic centers using the same camphorsultam chiral auxiliary.
- Liang, Bo,Carroll, Patrick J.,Joullie, Madeleine M.
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p. 4157 - 4160
(2007/10/03)
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- A practical method for N-acylation of bornane-2,10-sultam and 2-oxazolidinones
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The N-trimethylsilyl derivatives of (+)-bornane-2,10-sultam (10,10-dimethyl-5-thia-4-azatricyclo[5.2.1.03,7]decane 5,5-dioxide) and (R)-4-benzyl-2-oxazolidinone and 4-methyl-5-phenyl-2-oxazolidinone react with acid chlorides in refluxing benzen
- Thom,Kocienski
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p. 582 - 586
(2007/10/02)
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- On the Scope of Asymmetric Nitrile Oxide Cycloadditions with Oppolzer's Chiral Sultam. Total Syntheses of (+)-Hepialone, (-)-(1R,3R,5S)-1,3-Dimethyl-2,9-dioxabicyclooctane
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Cycloadditions of nitrile oxides with acryloyl derivatives of Oppolzer's chiral sultam produce stereoisomeric Δ2-isoxazolines in ratios of about 90/10 at 25 deg C.The major diastereomers can be isolated in pure form in 70-88percent yield.Synthe
- Curran, Dennis P.,Heffner, Timothy A.
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p. 4585 - 4595
(2007/10/02)
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- IRIDOIDS : ENANTIOSELECTIVE SYNTHESIS OF LOGANIN VIA AN ASYMMETRIC DIELS-ALDER REACTION
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Starting from (-)-camphor-10-sulfonic acid (5) the crystalline sultam 9 was readily prepared.TiCl4-mediated Diels-Alder addition of the N-crotonyl sultam 11 to cyclopentadiene, crystallization of the resulrting adduct 12 and subsequent reduction gave virtually pure (1S, 4R,5R, 6S)-1 together with recovered auxiliary 9.The loganin precursor 1 was transformed into norbonanone 20, which upon Baeyer-Villiger oxidation led to the suitably substituted cyclopentane 22 from which 1-B-O-methyl loganin aglucone (2) was readily available.
- Vandewalle, M.,Van der Eycken, J.,Oppolzer, W.,Vullioud, C.
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p. 4035 - 4044
(2007/10/02)
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