- Preparation method of fluorodesoxyribofuranose
-
The invention provides a preparation method of fluorodesoxyribofuranose. The structure of the fluorodesoxyribofuranose is represented by general formula 1 shown in the description; and the general formula 1, 1a:R = F, and R' = Me; and 1b:R = Me, and R' = F. The fluorodesoxyribofuranose prepared through the brand new preparation method can be used in researching of new medicines, or can be used in researches as a research model. The method adopts glyceraldehyde acetonide as a raw material and allows enantiomers in all intermediates to be effectively separated through a four-step reaction by adopting a rectification or distillation and re-crystallization technology, and a 2-posiion single optical isomer in the target product is directly constructed through an enol addition reaction, so the preparation of the target compound is smooth completed, and the method has the advantages of high yield, simple operation, and suitableness for promotion and application.
- -
-
Page/Page column 0126; 0127
(2016/10/09)
-
- PRODUCTION METHOD OF (2R)-2-FLUORO-2-C-METHYL-D-RIBONO-γ-LACTONE
-
PROBLEM TO BE SOLVED: To provide a production method of (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone. SOLUTION: A (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor containing various diastereomers can be produced by performing Reformatsky reaction using activated metal to a 2-fluoro-2-halopropionate derivative and a D-glyceraldehyde derivative. The obtained mixture containing the (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is subjected to deprotection and lactonizing under an acidic condition, is converted to a diastereomer mixture containing 2-fluoro-2-C-methyl-D-ribono-γ-lactone and is recrystallized, thereby inducing the mixture to (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone. COPYRIGHT: (C)2015,JPOandINPIT
- -
-
Paragraph 0128; 0129; 0130
(2016/11/07)
-
- A neighboring group participation strategy: Facile synthesis of 3,5-di-O-benzoyl-2-C-methyl-d-arabino-γ-lactone
-
A simple and efficient approach for the synthesis of 3,5-di-O-benzoyl-2-C-methyl-d-arabino-γ-lactone through a neighboring group participation mechanism is reported. This compound could be a useful precursor for the synthesis of nucleoside antiviral agents.
- Xie, Yuanchao,Zhang, Jian,Tian, Guanghui,Xu, Mingshuo,Hu, Tianwen,Jiang, Xiangrui,Shen, Jingshan
-
p. 4345 - 4348
(2015/06/22)
-
- A practical synthesis of (2R)-3,5-di-O-benzoyl-2-fluoro-2-C-methyl-d-ribono-γ-lactone
-
The title compound was synthesized in 23% overall yield using only one purification in four chemical steps. The key features of this practical synthesis include an asymmetric aldol condensation and an enzymatic hydrolysis to remove the major undesired iso
- Zhang, Pingsheng,Iding, Hans,Cedilote, Miall,Brunner, Stephan,Williamson, Thomas,Cleary, Thomas P.
-
experimental part
p. 305 - 312
(2009/08/15)
-