863324-53-2Relevant academic research and scientific papers
SCALEABLE PREPARATION OF POLYKETIDES
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Paragraph 0287-0290; 0358-0360, (2021/02/12)
Disclosed herein, inter alia, are methods of making polyketide compounds.
A acylation of the synthesis method of sulfur on behalf of the oxazolidone
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Paragraph 0025; 0026; 0027, (2019/01/08)
The invention discloses a method for acylation of the synthesis method of sulfur on behalf of the oxazolidone. Synthesis method of the invention, comprising the following steps: in the non-protic organic solvent, the compound III and under the action of a
Synthesis and Cytotoxicity Evaluation of C4- and C5-Modified Analogues of the α,β-Unsaturated Lactone of Pironetin
Huang, David S.,Wong, Henry L.,Georg, Gunda I.
supporting information, p. 520 - 528 (2017/04/10)
Pironetin is a natural product with potent antiproliferative activity that forms a covalent adduct with α-tubulin via conjugate addition into the natural product's α,β-unsaturated lactone. Although pironetin's α,β-unsaturated lactone is involved in its binding to tubulin, the structure–activity relationship at different positions of the lactone have not been thoroughly evaluated. For a systematic evaluation of the structure–activity relationships at the C4 and C5 positions of the α,β-unsaturated lactone of pironetin, twelve analogues of the natural product were prepared by total synthesis. Modifying the stereochemistry at the C4 and/or C5 positions of the α,β-unsaturated lactone of pironetin resulted in loss of antiproliferative activity in OVCAR5 ovarian cancer cells. While changing the C4 ethyl substituent with groups such as methyl, propyl, cyclopropyl, and isobutyl were tolerated, groups with larger steric properties such as an isopropyl and benzyl groups were not.
Synthesis and Fungicidal Activity of Simple Structural 1,3-Thiazolidine-2-Thione Derivatives
Chen, Ning,Du, Hongguang,Liu, Weidong,Wang, Shanshan,Li, Xinyao,Xu, Jiaxi
, p. 112 - 122 (2015/10/29)
A series of simple structural 1,3-thiazolidine-2-thione derivatives with various substituents on the S-, N-, 4-, and 5-positions was synthesized with high yields from various vicinal amino alcohols via two steps and screened for their antifungal activity. Bioassay results reveal that some thiazolidine-2-thione derivatives show strong antifungal activities against P. capsici, G. zeae, S. sclerotiorum, A. alternata, B. cinerea, or R. solani. The SAR analysis indicates that N-acyl substituted and 4-alkyl substituents can enhance the antifungal activity. Notably, 4-isopropyl-N-propionylthiazoldine-2-thione shows excellent activity against B. cinerea and G. zeae with IC50 values at 3.7 g/mL and 6.5 g/mL, respectively, and 4-isobutyl-N-propionylthiazoldine-2-thione shows remarkable fungicidal activity against R. solani, S. sclerotiorum, and G. zeae with IC50 values at 1.0 g/mL, 12.1 g/mL, and 11.0 g/mL, respectively. GRAPHICAL ABSTRACT.
Studies toward the total synthesis of sorangicins: A shortened synthesis of the dioxabicyclo[32.1]octane core
Michaelis, Lars,Schinzer, Dieter
, p. 951 - 954 (2014/05/06)
An access to the dioxabicyclo[3.2.1]octane core of sorangicin A was developed, using a keto lactone formation, a Mukaiyama-Michael reaction and an epoxide opening as the key steps. Georg Thieme Verlag Stuttgart - New York.
ANTI-CANCER POLYKETIDE COMPOUNDS
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, (2013/10/21)
Provided herein, inter alia, are anticancer polyketides. The uses of the polyketides described herein include treatment of cancer, for example, through regulation of the spliceosome and detection of spliceosome inhibition.
Structure of FD-895 revealed through total synthesis
Villa, Reymundo,Mandel, Alexander L.,Jones, Brian D.,La Clair, James J.,Burkart, Michael D.
, p. 5396 - 5399 (2013/01/15)
The total synthesis of FD-895 was completed through a strategy that featured the use of a tandem esterification ring-closing metathesis (RCM) process to construct the 12-membered macrolide and a modified Stille coupling to append the side chain. These stu
An improved synthesis of sitophilure
Lu, Cuifen,Nie, Junqi,Yang, Guichun,Chen, Zuxing
experimental part, p. 30 - 32 (2009/09/30)
The asymmetric synthesis of sitophilure was carried out in 8 steps, with 42% overall yield and 97% enantiomeric excess from propionaldehyde. The synthesis relied on an approach employing an asymmetric acyl-thiazolidinethione propionate aldol reaction to e
On the influence of chiral auxiliaries in the stereoselective cross-coupling reactions of titanium enolates and acetals
Baiget, Jessica,Cosp, Annabel,Gálvez, Erik,Gómez-Pinal, Loreto,Romea, Pedro,Urpí, Fèlix
, p. 5637 - 5644 (2008/09/21)
Titanium enolates from chiral N-propanoyl-1,3-thiazolidine-2-thiones containing bulky substituents at C4 turned out to be excellent platforms to get highly stereocontrolled cross-coupling reactions with acetals. Related oxazolidinethiones also afforded go
