97614-44-3

Usage

Uses

Used in Pharmaceutical Industry:
2-Deoxy-2-fluoro-alpha-D-arabinofuranosyl bromide 3,5-dibenzoate is used as a key intermediate in the synthesis of Clofarabine (C586890), a second-generation purine nucleoside analog. Clofarabine is an antimetabolite that inhibits DNA synthesis and resists deamination by adenosine deaminase, making it an effective antineoplastic agent. Its role in the synthesis of Clofarabine highlights its importance in the development of cancer treatments.
Additionally, 2-Deoxy-2-fluoro-alpha-D-arabinofuranosyl bromide 3,5-dibenzoate is related to the antibiotic Gentamicin, indicating its potential use in the development of new antibiotics or improvements to existing ones. This relationship suggests that the compound may have properties that contribute to the effectiveness of antibiotics, particularly in the context of treating bacterial infections.

Upstream product

• 97614-43-2 1,3,5-tri-O-benzoyl-2-deoxy-2-fluoro-α-D-arabinofuranose 
• 22224-41-5 1,3,5-tri-O-benzoyl-α-D-ribofuranoside 
• 97614-42-1 2-O-(imidazolylsulfonyl)-1,3,5-tri-O-benzoyl-α-D-ribofuranose 
• 491594-58-2 1,3,5-tri-O-benzoyl-2-deoxy-2-fluoro-β-D-arabinofuranose 
• 14215-97-5 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribofuranose 

Downstream Products

• 132723-16-1 (2R,3R,4S,5R)-4-Fluoro-2-hydroxymethyl-5-purin-7-yl-tetrahydro-furan-3-ol 
• 109304-16-7 9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)purine 
• 132723-15-0 C₂₄H₁₉FN₄O₅ 
• 132723-01-4 9-(3',5'-di-O-benzoyl-2'-deoxy-2'-fluoro-β-D-arabinofuranosyl)-9H-purine 
• 132723-14-9 C₂₄H₁₉FN₄O₅ 
• 128496-10-6 1-(3',5'-di-O-benzoyl-2'-deoxy-2'-fluoro-β-D-arabinofuranosyl)uracil 
• 97614-47-6 1-(3',5'-di-O-benzoyl-2'-deoxy-2'-fluoro-β-D-arabinofuranosyl)thymine 
• 97614-48-7 1-(2-deoxy-2-fluoro-3,5-di-O-benzoyl-α-D-arabinofuranosyl)thymine 
• 118373-61-8 2-amino-6-chloro-9-(3',5'-di-O-benzoyl-2'-deoxy-2'-fluoro-β-D-arabinofuranosyl)-9H-purine 
• 118373-60-7 2-amino-6-chloro-9-(3,5-di-O-benzoyl-2-deoxy-2-fluoro-α-D-arabinofuranosyl)-9H-purine 
• 194159-88-1 2,5,6-trichloro-1-(3,5-di-O-benzoyl-2-deoxy-2-fluoro-β-D-arabinofuranosyl)benzimidazole 
• 743467-44-9 8-(3,5-di-O-benzoyl-2-deoxy-2-fluoro-β-D-arabinofuranosyl)-2-[(2-methyl-1-oxopropyl)amino]imidazo[1,2-a]-1,3,5-triazin-4(8H)-one 
• 909101-46-8 4-chloro-7-(2-deoxy-3,5-di-O-benzoyl-β-D-arabinofuranosyl)-5-fluoro-7H-pyrrolo[2,3-d]pyrimidine 
• 916987-55-8 p-chlorophenyl 2-deoxy-2-fluoro-1-thio-β-D-arabinofuranoside 

Relevant academic research and scientific papers

S-ANTIGEN TRANSPORT INHIBITING OLIGONUCLEOTIDE POLYMERS AND METHODS

Various embodiments provide STOPS? polymers that are S-antigen transport inhibiting oligonucleotide polymers, processes for making them and methods of using them to treat diseases and conditions. In some embodiments the STOPS? modified oligonucleotides include an at least partially phosphorothioated sequence of alternating A and C units having modifications as described herein. The sequence independent antiviral activity against hepatitis B of embodiments of STOPS? modified oligonucleotides, as determined by HBsAg Secretion Assay, is an EC50 that is less than 100 nM.

METTL3 MODULATORS

Provided are compounds of Formula (I') or (II'), or pharmaceutically acceptable salts thereof, and methods for their use and production.

Synthesis of Rovafovir Etalafenamide (Part IV): Evolution of the Synthetic Process to the Fluorinated Nucleoside Fragment

Fluorinated nucleoside 1 is a key starting material in the synthesis of rovafovir etalafenamide (2), a novel nucleotide reverse transcriptase inhibitor under development at Gilead Sciences for the treatment of HIV. While an initial manufacturing route enabled the production of 1 to support clinical development, alternative approaches were explored to further enhance manufacturing effectiveness, improve processing time, reduce cost, and minimize the environmental impact. Toward this end, two new routes were developed to a key synthetic intermediate, which was converted to 1 using a new protecting group strategy. The new chemistry led to improvements in the manufacturing process while reducing the overall process mass intensity (PMI).

2,4,7-SUBSTITUTED-7-DEAZA-2'-DEOXY-2'-FLUOROARABINOSYL NUCLEOSIDE AND NUCLEOTIDE PRO-DRUGS AND USES THEREOF

The present disclosure is concerned with 2,4,7-substituted-7-deaza-2'-deoxy-2'- fluoroarabinosyl nucleoside and nucleotide prodrugs that are capable of inhibiting viral infections and methods of treating viral infections such as, for example, human immunodeficiency virus (HIV), human papillomavirus (HPV), herpes simplex virus (HSV), human cytomegalovirus (HCMV), chicken pox, infectious mononucleosis, mumps, measles, rubella, shingles, ebola, viral gastroenteritis, viral hepatitis, viral meningitis, human metapneumovirus, human parainfluenza virus type 1, parainfluenza virus type 2, parainfluenza virus type 3, respiratory syncytial virus, viral pneumonia, Chikungunya virus (CHIKV), Venezuelan equine encephalitis (VEEV), dengue (DENV), influenza, West Nile virus (WNV), zika (ZIKV), 229E, NL63, OC43, HKU1, Middle East respiratory syndrome coronavirus (MERS-CoV), severe acute respiratory syndrome coronavirus (SARS-CoV), and severe acute respiratory syndrome coronavirus disease 2019 (SARS-CoV-2), using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

ANTIVIRAL DRUG

PROBLEM TO BE SOLVED: To provide a nucleic acid analog having excellent antiviral activity (particularly anti-hepatitis B virus activity). SOLUTION: The invention provides a compound represented by the formula (I) in the figure, where each symbol is as defined in the specification, or a salt thereof. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS

The present invention is directed to compounds of the formulae I, II and III as shown below wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Green synthesizing technology of clofarabine

The invention relates to a green synthesizing technology of clofarabine which comprises the following steps: (the structural formula is shown in the description), dissolving a compound which is shownin formula II into an organic solvent, adding 40% of hydrobromic acid and tetrabutylammonium fluoride in an ice bath, performing stirring reaction for 3 hours, adding triethylamine trihydrofluoride and continuing the stirring reaction for 2 to 3 hours to obtain a compound which is shown in formula I; (2) dissolving a compound which is shown in formula III into acetonitrile, adding potassium tert-butoxide, calcium hydride and tert-butyl alcohol, heating to 60 DEG C, reacting for 1 hour, adding the compound which is shown in the formula I, keeping at 60 DEG C and continuing reacting for 10 hoursto obtain a compound which is shown in formula IV; (3) removing Bz in the compound which is shown in the formula IV under an alkaline condition to obtain a compound which is shown in a formula V, namely the clofarabine.

Compatibility of 5-ethynyl-2′F-ANA UTP with: In vitro selection for the generation of base-modified, nuclease resistant aptamers

A modified nucleoside triphosphate bearing two modifications based on a 2′-deoxy-2′-fluoro-arabinofuranose sugar and a uracil nucleobase equipped with a C5-ethynyl moiety (5-ethynyl-2′F-ANA UTP) was synthesized. This nucleotide analog could enzymatically

ATG7 INHIBITORS AND THE USES THEREOF

Disclosed are chemical entities which are compounds of formula (I) : or a pharmaceutically acceptable salt thereof, wherein R1, R2, and Ra have the values described herein. Chemical entities according to the disclosure can be useful as inhibitors of ATG7. Further provided are pharmaceutical compositions comprising a chemical entity of the disclosure and methods of using the compositions in the treatment of cancer.

METHOD FOR PREPARING PRECURSOR OF GENE EXPRESSION PROBE

A method for preparing a precursor of gene expression probe is revealed. First prepare 2-deoxy-2-fluoro-3,5-di-O-benzoyl-[alpha]-D-arabinofuranosyl bromide and 2,4-bis-O-(trimethylsilyl)-5-bromouracil respectively. Then use 2-deoxy-2-fluoro-3,5-di-O-benzo