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Method for preparing duloxetine chiral intermediate through microbial conversion

A technology for microbial transformation and chiral intermediates, applied in the direction of microorganism-based methods, biochemical equipment and methods, microorganisms, etc., can solve problems such as non-ideal pathways, and achieve easy large-scale industrial production, high yield, and large-scale Cultivate easy effects

Active Publication Date: 2015-02-11
瑞博(杭州)医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Therefore, the lipase resolution racemate method is not an ideal way for the industrialized preparation of (S)-3-hydroxyl-3-(2-thienyl)propionitrile

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The CGMCC No. 2266 strain was inoculated into the slant medium, and cultured at 30°C for 4-6 days to obtain the slant surface of the bacteria. An inoculation loop was taken from the slant of the bacteria with an inoculation needle and inoculated into a 250 mL Erlenmeyer flask containing 100 mL of liquid medium, and cultured at 30 °C and 180 r / min for 24 h to obtain a seed liquid. Inoculate 10 mL of seed solution (the inoculum volume is calculated as 10% of the medium volume fraction) into a 250 mL Erlenmeyer flask containing 100 mL of liquid medium, and culture it at 30 °C and 180 r / min for 24 h to obtain a fermentation broth. The fermentation broth is centrifuged to obtain enzyme-containing bacterial cells.

[0039] The determination of the dry weight of the bacteria is to take a small part of the wet bacteria containing the enzyme cells after centrifuging the fermentation broth, and dry it at 120 °C for 48 hours to a constant weight, measure the weight of the dry cell...

Embodiment 2

[0044] The CGMCC No. 2266 strain was inoculated into the slant medium, and cultured at 30°C for 4-6 days to obtain the slant surface of the bacteria. An inoculation loop was taken from the slant of the bacteria with an inoculation needle and inoculated into a 250 mL Erlenmeyer flask containing 100 mL of liquid medium, and cultured at 30 °C and 180 r / min for 24 h to obtain a seed liquid. Inoculate 10 mL of seed liquid (the inoculum amount is calculated as 10% of the medium volume) into a 250 mL Erlenmeyer flask containing 100 mL of liquid medium, and culture at 30 °C and 180 r / min for 24 h to obtain a fermentation broth. The fermented liquid is centrifuged to obtain enzyme-containing bacterium cells, and the dry weight of the enzyme-containing bacterium cells in every liter of fermented liquid is 50 grams.

[0045] Add the wet cells obtained after centrifugation of the above-mentioned 400 milliliters of fermented liquid into ten portions of Erlenmeyer flasks each containing 100...

Embodiment 3

[0049] Saccharomyces cerevisiae CGMCC No. 2266 was inoculated into the slant medium, and cultured at 30°C for 4-6 days to obtain the slant. An inoculation loop was taken from the slant of the bacteria with an inoculation needle and inoculated into a 250 mL Erlenmeyer flask containing 100 mL of liquid medium, and cultured at 30 °C and 180 r / min for 24 h to obtain a seed solution. Inoculate 10 mL of seed solution (the inoculum amount is calculated as 10% of the medium volume) into a 250 mL Erlenmeyer flask containing 100 mL of liquid medium, and culture it at 30 °C and 180 r / min for 24 h to obtain a fermentation broth. The fermented liquid is centrifuged to obtain enzyme-containing bacterium cells, and the dry weight of the enzyme-containing bacterium cells in every liter of fermented liquid is 50 grams.

[0050] Add the wet cells obtained after centrifugation of the above 400 ml fermentation broth to five parts of Erlenmeyer flasks each containing 100 mL of pH7.0 phosphate buff...

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Abstract

The invention provides a method for preparing duloxetine chiral intermediate (S)-3-hydroxyl-3-(2-thineyl) propanenitrile through microbial conversion. The method comprises the following step of: converting 3-hydroxyl-3-(2-thineyl) propanenitrile into the (S)-3-hydroxyl-3-(2-thineyl) propanenitrile under the catalysis of enzyme-containing thallus cells obtained by fermentation of saccharomyces cerevisiae CGMCC No. 2266. The method has the advantages of mild reaction conditions, easiness and convenience for operation, low cost, high product yield, high purity and suitability for large-scale industrial production.

Description

technical field [0001] The invention belongs to the field of microbial transformation, in particular to a method for preparing duloxetine chiral intermediate (S)-3-hydroxyl-3-(2-thienyl)propionitrile by microbial transformation. Background technique [0002] (S)-3-hydroxy-3-(2-thienyl) propanenitrile ((S)-3-hydroxy-3-(2-thienyl) propanenitrile), CAS accession number: 591727-36-5, molecular formula C 7 h 7 NOS, molecular weight 153. (S)-3-Hydroxy-3-(2-thienyl)propionitrile is an important intermediate in the synthesis of antidepressant duloxetine. Duloxetine is a novel antidepressant that acts as a dual inhibitor of serotonin and norepinephrine reuptake. At present, it has been found that it can not only treat depression, but also can be used to treat stress urinary incontinence and diabetic peripheral neuropathic pain. It also has a certain effect on chronic pain associated with depression. [0003] Ahmed Kamal, G. B. et al. disclose a route for the preparation of duloxe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12P17/00C12R1/865
Inventor 沈文和欧志敏车大庆
Owner 瑞博(杭州)医药科技有限公司
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