Aryl-substituted acyclic enediyne compounds
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Example
Example 1
Synthesis of 4-trimethylsilyl-1-chorobuten-3-yne (a1)
4-trimethylsilyl-1-chorobuten-3-yne (a1) was synthesized using cis-1,2-dichloroethylene and (trimethylsilyl)acetylene as the starting materials according to Method A of the above-described General Synthesis Procedures I, and gives a brown oil in 40% yield.
Example
Example 2
Synthesis of 2-(2-trimethylsilyl-1-ethynyl)iodobenzene (a2)
The title compound was synthesized as a yellow oil in 54% yield using 1,2-diiodobenzene and (trimethylsilyl)acetylene as the starting materials according to Method A of the above-described General Synthesis Procedures I.
Example
Example 3
Synthesis of 2-ethynylbenzonitrile (a3)
The title compound may be prepared from compound (a2) of Example 2 in two steps according to the above synthesis scheme. According to Method B of the above-described General Synthesis Procedures I, compound (a2) is converted to 2-(2-trimethylsilylethynyl)benzonitrile, which is then dissolved into dry methanol with K2CO3 to give a white solid in 73% yield (Method C of the above-described General Synthesis Procedures I).
Alternatively, 2-ethynylbenzonitrile (a3) may be prepared according to the procedures set forth in M. J. Wu et al. (1999), Organic Letters, 1 (5):767-768, which is incorporated herein by reference in its entirety. Specifically, palladium-catalyzed coupling reaction of trimethylsilylacetylene with 1,2-diiodobenzene produced 2-(2-trimethylsilylethynyl)iodobenzene in 58% yield; 2-(2-trimethylsilylethynyl)iodobenzene was then coupled with Zn(CN)2 using palladium(0) as a catalyst to give 2-(2-trimethylsilylethynyl)benzonitri
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Abstract
- R1═R2═H; or R1 and R2 together form a moiety represented by the formula
- R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R represents a substituted or unsubstituted aryl group having 3-30 carbon atoms;
- with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1═R2═H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1═R2═H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.
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