30361-18-3

Upstream product

• 729596-46-7 3,5-di-O-benzoyl-2-C-methyl-D-ribono-γ-lactone 
• 492-30-8 2-C-methyl-D-ribono-1,4-lactone 
• 98-88-4 benzoyl chloride 

Downstream Products

• 15397-15-6 1,2,3,5-tetra-O-benzoyl-2-C-methyl-β-D-ribofuranose 
• 23643-36-9 2′,3′,5′-tri-O-benzoyl-2′-C-methyluridine 
• 1199809-23-8 ((2R,3R,4R,5R)-3-(benzoyloxy)-5-chloro-4-fluoro-4-methyltetrahydrofuran-2-yl)methyl benzoate 
• 817204-32-3 (2R,3R,4R,5R)-5-(4-benzamido-2-oxopyrimidin-1(2H)-yl)-2-((benzoyloxy)methyl)-4-fluoro-4-methyltetrahydrofuran-3-yl benzoate 

Relevant academic research and scientific papers

Technology for preparing sofosbuvir intermediate

A technology for preparing a sofosbuvir intermediate represented by formula 1 comprises the following steps: (a) reducing a compound 2 by sodium borohydride to generate a compound 3; (b) reacting thecompound 3 with a methanol-hydrochloric acid solution to generate a compound 4; (c) carrying out a fluorination reaction on the compound 4 and a fluorination reagent in a reaction solvent at -10 to -65 DEG C under the protection of nitrogen, and post-treating a reaction solution after the reaction is fully carried out in order to obtain a compound 5; (d) cooling an n-hexane or petroleum ether or cyclohexane solution of the compound 5 to -5-5 DEG C under the protection of nitrogen, adding thionyl chloride, slowly dropwise adding methanol or ethanol at a controlled temperature of -5-5 DEG C, rising the temperature to 10-40 DEG C after the dropwise addition, continuously performing stirring until the reaction is completed , and removing the solvent to obtain a compound 6; and (e) condensing the compound 6 and a compound 7, and carrying out hydrolysis treatment to obtain the target product which is the compound 1. The preparation technology has the characteristics of high yield, convenience and safety in operation, less discharge of three wastes, low production cost, and suitableness for industrial production.

Synthesis process of (2R')-2'-deoxyl-2'-fluoro-2'-methyluridine

The invention discloses a synthesis process of (2R')-2'-deoxyl-2'-fluoro-2'-methyluridine, relates to the technical field of synthesis of medicines, and solves the technical problems of high cost andlow product yield of the existing process. According to the synthesis process, sodium borohydride or potassium borohydride is used for reducing ribose lactone, so that an expensive reductive reagent which is sodium dihydro-bis-(2-methoxyethoxy)aluminate or lithium tri-tert-butoxyaluminum hydride is not used, and the cost is greatly reduced; N,O-bis(trimethylsilyl)acetamide is used as a silicon etherification reagent, so that the yield of glycosylation reaction is increased; the product yield can reach 85-90% and is far higher than that in route III by 58%; the product yield is obviously increased; hydroxyl at the 5' site is protected, so that side reaction in ring-closing reaction can be avoided; meanwhile, a common polar solvent which is dimethylformamide is used; the product yield undercatalysis of sodium hydrogen carbonate can reach 87-92%. The synthesis process is easy to operate; the process condition is more easily controlled; the cost is reduced; the synthesis process is applicable to large-batch production.

Process for the preparation of ribofuranose derivatives

The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of formula (I): useful in the synthesis of nucleotides.

PROCESS FOR THE PREPARATION OF RIBOFURANOSE DERIVATIVES

The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of Formula (I) useful in the synthesis of nucleotides.