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5-fluorocytidine complete cell enzymatic synthesis method

A flucytosine nucleoside, enzymatic synthesis technology, applied in the field of synthesis of 5-fluorocytosine nucleoside, can solve the problems of long time-consuming, unfavorable large-scale continuous production, low overall yield, etc., to achieve increased yield, Ease of collection and shortened time

Inactive Publication Date: 2007-07-11
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The technical problem to be solved by the present invention is to provide a whole-cell enzymatic synthesis method of 5-fluorocytosine nucleoside to solve the problem that the overall yield in the existing chemical method and enzymatic synthesis is lower than 25%, which takes a long time and is not conducive to Disadvantages of industrialized large-scale continuous production

Method used

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  • 5-fluorocytidine complete cell enzymatic synthesis method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] 1mL 50mmol / / L NaH with pH=8 2 PO 4 Add D-D4T 5.6mg (25 mmol / L), 5-FC 6.4mg (50mmol / L), and 1.2g Lactobacillus to the buffer solution in a 5mL Erlenmeyer flask, and seal it with multiple layers of gauze. The reaction was shaken at 120r / min in an air shaker at 40°C for 12.5h. After the reaction was completed, the reaction system was frozen and stored at -20°C to terminate. After the sample was thawed, it was centrifuged at 10,000 r / min for 15 minutes to remove the whole cells, and the obtained supernatant was filtered and used for HPLC detection.

Embodiment 2

[0019] 1mL 50mmol / / L NaH with pH=6.85 2 PO 4 5.6 mg (25 mmol / L) of D-D4T, 6.4 mg (50 mmol / L) of 5-FC, and 2 g of Lactobacillus were added to the buffer solution in a 5 mL Erlenmeyer flask, which was sealed with multiple layers of gauze. The reaction was shaken at 120r / min in an air shaker at 40°C for 12.5h. After the reaction was completed, the reaction system was frozen and stored at -20°C to terminate. After the sample was thawed, it was centrifuged at 10,000 r / min for 15 minutes to remove the whole cells, and the obtained supernatant was filtered and used for HPLC detection.

Embodiment 3

[0021] 1mL 50mmol / / L NaH with pH=6.85 2 PO 4 Add D-D4T 5.6mg (25 mmol / L), 5-FC 6.4mg (50 mmol / L), and 1.2g Lactobacillus into a 5mL Erlenmeyer flask to the buffer, and seal it with multiple layers of gauze. The reaction was shaken at 120r / min in an air shaker at 40°C for 100h. After the reaction was completed, the reaction system was frozen and stored at -20°C to terminate. After the sample was thawed, it was centrifuged at 10,000 r / min for 15 minutes to remove the whole cells, and the obtained supernatant was filtered and used for HPLC detection.

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Abstract

The invention discloses a whole-cell enzymatic synthesizing method of 5-flucytosine nucleoside, which is characterized by the following: reacting buffer with N-deoxyribose transferase and 5-flucytosine to exchange alkaline under 37-50 deg. c for 10-20h; obtaining the product similar to flucytosine to 49. 4% within 20h.

Description

technical field [0001] The invention relates to a method for synthesizing 5-fluorocytosine nucleoside, in particular to a whole-cell enzymatic synthesis method for 5-fluorocytosine nucleoside. Background technique [0002] D-D4FC (β-D-2',3'-didehydrodideoxy-5-fluorocytidine nucleoside) is a new type of anti-HIV nucleoside drug. Taken once / day or twice / day, it can effectively inhibit HIV protobacteria, anti-AZT (zidofuridine, 3'-deoxy-3'-azidethymidine) strains and anti-3TC (Lami Furidine, 3'-thiocytidine) strains and HIV variant strains resistant to other NRTIs (nucleoside reverse transcriptase inhibitors), NNRTIs (non-nucleoside reverse transcriptase inhibitors), PIs (protease inhibitors) drugs ( Antimicrob Agents Chemother, 2002, 46(5): 1394-1401.). So far, no new HIV mutant strains have been found in patients taking D-D4FC. Importantly, the combination of D-D4FC and other virus inhibitors except DDI (2', 3'-dideoxyinosine) has no mutual inhibitory effect and almost no ...

Claims

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Application Information

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IPC IPC(8): C12P19/40
Inventor 朱利民戚娜
Owner DONGHUA UNIV
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