- ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS
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The disclosure relates to anti-cancer compounds which are anti-cancer PARP inhibitors of formula Al, A2, A3 or A4 conjugated by a linker to a steroid, whereby the steroid targets the conjugate to the nucleus, as well as to methods for their preparation and use. (I)
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Page/Page column 147-149
(2021/05/21)
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- An efficient synthesis of 5α-androst-1-ene-3,17-dione
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5α-Androst-1-ene-3,17-dione (5) as a prodrug of 1-testosterone (4) was prepared in four steps from 17β-Acetoxy-5α-androstan-3-one (stanolone acetate) (1) in high yield. Thus, stanolone acetate (1) was brominated in the presence of hydrogen chloride in acetic acid to give 17β-acetoxy-2-bromo-5α-androstan-3-one (2), which underwent dehydrobromination using lithium carbonate as base with lithium bromide as an additive to give 17β-acetoxy-5α-androst-1-en-3-one (3) in almost quantitative yield with 97% of purity. Compound (3) was hydrolyzed with sodium hydroxide to give 17β-hydroxy-5α-androst-1-en-3-one (4,1-testosterone), which was oxidized with chromium trioxide to afford 5α-androst-1-ene-3,17-dione (5). The overall yield of 5 was 78.2% with purity of 99%. In this method, the formation of 4-ene was diminished when 1-ene was introduced, and its mechanism was also discussed.
- Zhang, Huyue,Qiu, Zhuibai
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p. 1088 - 1090
(2007/10/03)
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- HIO3 and I2O5: Mild and selective alternative reagents to IBX for the dehydrogenation of aldehydes and ketones
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Economic and convenient: Iodic acid (1) and iodine pentoxide (2) form complexes 3 and 4, respectively, with DMSO when heated at 80°C for 1 h. The complexes are efficient agents for the dehydrogenation of ketones and aldehydes at 45-65°C. X-ray crystallographic analysis (see picture) shows that the iodine pentoxide. DMSO complex 4 self-assembles into a remarkable helix in the solid state.
- Nicolaou,Montagnon, Tamsyn,Baran, Phil S.
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p. 1386 - 1389
(2007/10/03)
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- A facile synthesis of 1β-hydroxytestosterone
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A convenient synthesis of androst-4-en-1β,17β-diol-3-one (1β-hydroxytestosterone, 1) from 5α-androst-3-on-17β-benzoate (dihydrotestosterone benzoate) is described.
- Sharma, P K,Akhila, A
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p. 554 - 556
(2007/10/02)
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