63930-46-1Relevant articles and documents
Stereoselective 1,5-rearrangement of vinylketene-N,O-acetals: Novel vinylogous Ferrier reaction
Inui, Masaharu,Hosokawa, Seijiro,Nakazaki, Atsuo,Kobayashi, Susumu
, p. 3245 - 3248 (2005)
Vinylketene-N,O-acetals underwent Lewis acid-induced 1,3- or 1,5-rearrangement to afford the corresponding C-alkylated products. 1,5-Rearrangement proceeded predominantly in dichloromethane, and it is quite interesting to achieve an unprecedented high degree of asymmetric induction in such a remote position. Crossover experiments indicated that the reaction proceeded through an ion pair intermediate.
6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
-
Paragraph 0890, (2021/11/13)
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Progress toward the total synthesis of mirabalin isomers
Echeverria, Pierre-Georges,Pons, Amandine,Prévost, Sébastien,Férard, Charlène,Cornil, Johan,Guérinot, Amandine,Cossy, Janine,Phansavath, Phannarath,Ratovelomanana-Vidal, Virginie
, p. 44 - 68 (2019/04/17)
Key fragments of the cytotoxic marine macrolide mirabalin have been synthesized, by using a flexible strategy based on asymmetric reductions to control the hydroxy- and carbamate-bearing stereocenters. In particular, ruthenium or rhodium-mediated asymmetric hydrogenation and transfer hydrogenation were used in combination with a dynamic kinetic resolution to control two contiguous stereocenters in a single step.
SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE
-
Paragraph 0468, (2017/04/14)
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
Substituted heteroaryl compound and composition thereof, and uses of substituted heteroaryl compound and composition thereof
-
Paragraph 1055; 1056; 1057; 1058, (2017/04/29)
The present invention provides a substituted heteroaryl compound and a composition thereof, and uses of the substituted heteroaryl compound and the composition, wherein the compound is a compound represented by a formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound represented by the formula (I). The present invention further provides a pharmaceutical composition containing the compound, wherein the pharmaceutical composition can regulate activity of protein kinases, particularly Aurora kinases and JAK kinases, and can be used for prevention, treatment, therapy and alleviation of protein kinases, particularly Aurora kinases and JAK kinase activity mediated diseases or disorders.
Total synthesis of odoamide, a novel cyclic depsipeptide, from an Okinawan marine cyanobacterium
Kaneda, Masato,Sueyoshi, Kosuke,Teruya, Toshiaki,Ohno, Hiroaki,Fujii, Nobutaka,Oishi, Shinya
, p. 9093 - 9104 (2016/10/07)
Odoamide is a novel cyclic depsipeptide with highly potent cytotoxic activity isolated from the Okinawan marine cyanobacterium Okeania sp. It contains a 26-membered macrocycle composed of a fatty acid moiety, a peptide segment and isoleucic acid. Four pos
Callipeltosides A, B and C: Total Syntheses and Structural Confirmation
Frost, James R.,Pearson, Colin M.,Snaddon, Thomas N.,Booth, Richard A.,Turner, Richard M.,Gold, Johan,Shaw, David M.,Gaunt, Matthew J.,Ley, Steven V.
supporting information, p. 13261 - 13277 (2015/09/15)
Since their isolation almost 20 years ago, the callipeltosides have been of long standing interest to the synthetic community owing to their unique structural features and inherent biological activity. Herein we present our full research effort that has led to the synthesis of these molecules. Key aspects of our final strategy include 1) synthesis of the C1-C9 pyran core (5) using an AuCl3-catalysed cyclisation; 2) formation of C10-C22 vinyl iodide (55) by sequential bidirectional Stille reactions and 3) diastereoselective union of these advanced fragments by means of an alkenylzinc addition (d.r.=91:9 at C9). The common callipeltoside aglycon (4) was completed in a further five steps. Following this, all three sugar fragments were appended to provide the entire callipeltoside family. In addition to this, D-configured callipeltose B was synthesised and appended to the callipeltoside aglycon. The 1H NMR spectrum of this molecule was found to be significantly different to the natural isolate, further supporting our assignment of callipeltoside B (2). Easy as A, B, C: The entire callipeltoside family of natural products have been synthesised in a highly convergent manner. This account details our full research effort and presents further evidence to aid in the stereochemical assignment of the glycosidic linkages present in callipeltosides B and C (see scheme).
DIHYDROPYRONE COMPOUNDS AND HERBICIDES COMPRISING THE SAME
-
Paragraph 0088, (2014/06/23)
The present invention provides a compound having an excellent efficacy for controlling weeds. A dihydropyrone compound of formula (I): wherein m is 1, 2 or 3; n is an integer of any one of 1 to 5; X represents O, S, S(O) or S(O)2; R1 /sup
Synthesis of a C1-C11 fragment of Zincophorin using planar chiral, neutral π-allyl iron complexes
Cooksey, John P.
supporting information, p. 5117 - 5126 (2013/08/23)
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
Efficient synthesis of the C1-C13 fragment of bistramide A
Tomas, Loic,Bechet, Thibault,Jeanneau, Erwann,Gueyrard, David,Goekjian, Peter G.
scheme or table, p. 215 - 218 (2012/03/26)
Herein we report an efficient synthesis of the C1-C13 fragment of bistramide A from (S)-1,2,4-butanetriol and Roche ester in 14 steps and 13% overall yield. Georg Thieme Verlag Stuttgart - New York.