- PRODRUGS OF ABIRATERONE
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The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers, or pharmaceutically acceptable salt(s) thereof as prodrugs of abiraterone. The present invention also describes method of making such compounds, pharmaceutical compositions comprising such compounds and the use of the compounds of formula (I).
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Page/Page column 30
(2021/05/29)
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- PROCESS FOR PREPARING RHODANINE-3-ACETIC ACID: A KEY INTERMEDIATED OF EPALRESTAT
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A process for preparation of (4-oxo-2-thioxo-1,3-thiazolidin-3-yl) acetic acid comprising: (a) reaction of compound of formula (VIII) wherein Y is Cl, Br, I, OTs, OMs and R is C1-8 alkyl, benzyl, cycloalkyl, phenyl, substituted phenyl and their like; with a compound of formula (VIIIA) wherein M is K, Na or Li, preferably K; R1 is C1-4 alkyl, benzyl, C1-C8 cycloalkyl, phenyl and their like, in aqueous medium to give a compound of formula (IX) (b) cyclizing a compound of formula (IX) using a base to give a compound of formula (X) in a solvent. (c) hydrolyzing (X) using aqueous mineral acid.
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Page/Page column 7
(2008/06/13)
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- Peptide Side-Arm Derivatives of Lariat Ethers and Bibracchial Lariat Ethers: Syntheses, Cation Binding Properties, and Solid State Structural Data
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Aza-18-crown-6 and 4,13-diaza-18-crown-6 derivatives having one or two side arms have been prepared.The side arms are of the form >N-Gly-AA-OMe, where "AA" is an amino acid.The 18-membered ring compounds were prepared by alkylation of aza-18-crown-6 as follows: Gly-Gly-OMe (14, 57percent, mp 42-43 deg C); Gly-Ile-OMe (15, 50percent); Gly-Val-OMe (16, 56percent).Two-armed compounds were obtained by alkylation of 4,13-diaza-18-crown-6 as follows: Gly-Gly-OMe (18, 58percent, mp 118-119 deg C); Gly-Ala-OMe (19, 50percent, mp 62-63 deg C); Gly-Phe-OMe (20, 65percent, oil); Gly-Leu-OMe (21, 51percent, mp 72-73 deg C); Gly-Ile-OMe (22, 60percent, oil); Gly-Val-OMe (23, 59percent, oil).Sodium iodide complexes of 18, 19, and 20 were isolated.Solid state structural data are reported for 18 and its sodium complex, as well as its potassium complex that was reported in preliminary form (ref 9f).Compound 18 crystallizes in the triclinic space group P1 with cell constants a = 9.0210 (8), b= 10.4768 (15), and c = 15.357 (2) Angstroem, α = 87.457 (12) deg, β = 87.119 (10) deg, γ = 68.042 (9) deg, and Z = 2 for Dc = 1.286 g cm-3.Least-squares refinement based on 4034 observed reflections led to a final conventional R value of 0.041.The sodium iodide complex of 18 crystallizes in the monoclinic space group P21/c with cell constants a = 9.732 (3), b = 17.710 (2), and c = 38.848 (3) Angstroem, β = 96.99 (2) deg, and Z = 8 for Dc = 1.430 g cm-3.Least-squares refinement based on 5512 observed reflection led to a final conventional R value of 0.041.The potassium iodide complex of 18 crystallizes in the monoclinic space group C2/c with cell constans a = 15.656 (4), b = 14.752 (3), and c = 26.784 (3) Angstroem, β = 90.01 (2), and Z = 8 for Dc = 1.474 g cm-3.Least-squares refinement based on 2595 observed reflections led to a final conventional R value of 0.035.There are two crystallographically independent molecules in each of the three crystal structures.The sodium and potassium complexes are compared to other BiBLE complexes and to cryptates.Cation binding affinities for these compounds have been assessed in anhydrous methanol and are reported here for Na+ and K+ cations.
- White, Banita D.,Mallen, Jesus,Arnold, Kristin A.,Fronczek, Frank R.,Gandour, Richard D.,et al.
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p. 937 - 947
(2007/10/02)
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