4'-halogen containing nucleotide and nucleoside therapeutic compositions and uses related thereto
A composition and compound technology, applied in the directions of medical preparations containing active ingredients, sugar derivatives, aerosol delivery, etc.
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example 1
[1883] Conjugate preparation
[1884]Monophosphate and diphosphate prodrugs have been prepared by several groups. See Jessen et al., "Bioreversible Protection of Nucleoside Diphosphates", "Angewandte Chemie-International Edition English" 2008, 47(45), 8719-8722, The above references are hereby incorporated by reference. To prevent the cleavage of P-O-P anhydride bonds, rapidly cleaved side groups (e.g., bis-(4-acyloxybenzyl)-nucleoside diphosphate (BAB-NDP) deacylated by endogenous esterases) are utilized at the A negative charge is created on the diphosphate. See also Routledge et al., "Synthesis, Bioactivation and Anti-HIV Activity of 4-Acyloxybenzyl-bis(nucleoside-5'-yl) phosphate (nucleosid-5′-yl)Phosphates)”, “Nucleosides & Nucleotides” 1995, 14(7), 1545-1558 and Meier et al., “2′,3′-Dideoxy-2′ ,Comparative study of bis(benzyl)phosphate triesters of 3′-didehydrothymidine (d4T) and cycloSal-d4TMP-hydrolysis, mechanistic insight and anti-HIV activity ,3′-dideoxy-2′,3′-...
example 2
[1887] General procedure for base coupling
[1888] Prepare persilylation under nitrogen in a round bottom flask containing dry nucleobase (15.5 mmol), chlorotrimethylsilane (12.21 mmol) and bis(trimethylsilyl)amine (222 mmol) nucleobase. The mixture was refluxed overnight (16 hours) with stirring until all solids had dissolved. The mixture was cooled to room temperature and volatiles were removed by rotary evaporation followed by high vacuum to obtain persilylated nucleobases. This compound was used immediately in the next step.
[1889] Freshly prepared persilylated nucleobase (15.50 mmol) was dissolved in 1,2-dichloroethane (50 mL) or chlorobenzene (50 mL) with stirring under nitrogen at room temperature. A solution of β-D-ribofuranose 1,2,3,5-tetraacetate (7.75mmol) in 1,2-dichloroethane (50mL) or chlorobenzene (50mL) was added to the Stir in the mixture.
[1890] To this mixture was added SnCl dropwise via syringe 4 (11.63 mmol), and the mixture was stirred at room ...
example 3
[1892] General Cytosine Analog Conjugation
[1893] in N 2 , with N 4 - A flask of benzoyl-protected cytosine analogue (0.793 mmol) was added bis(trimethylsilyl)amine (8.45 mmol) and ammonium sulfate (0.02 mmol). The flask was heated at reflux for 2 hours, and after cooling to room temperature, the solvent was removed in vacuo and further dried under high vacuum for 1 hour. The residue was dissolved in dry chlorobenzene (10 ml), and β-D- or β-L-ribofuranose 1,2,3,5-tetraacetate (0.53 mmol) was added. Then, add SnCl dropwise 4 (0.27ml, 2.3mmol). After stirring at room temperature for 1 hour, it was heated to 60° C. overnight. After cooling to 0 °C, solid sodium bicarbonate (0.85 g) was added followed by EtOAc (5 mL). It was allowed to stir for 15 minutes, and then water (0.5 mL) was added slowly. Insoluble material was filtered off and washed with more EtOAc (2.5 mL). The filtrate was washed once with water, once with brine, and dried (Na 2 SO 4 ) and concentrated in ...
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