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Liquid-liquid extraction equipment application in organic medium enzymatic reaction drug synthesis

by:Deyuan      2020-09-05
Organic medium in the process to enzymatic esterification and transesterification, according to the principle of thermodynamics, a kind of reactant alcohol or acid enantiomers easy to participate in the reaction, while another enantiomer alcohol or acid is not easy to participate in the reaction so as to realize optical resolution.
( 1) Break up turn ester reaction down drug
2 Amino propanol is intermediates for the synthesis of ofloxacin, its ( S) ( +) Type of isomer is pharmacological activity. Wei etc with ClCO2Et first to protect amino, then use of pancreatic lipase in ethyl acetate as catalyst for ester reaction, control of reaction type R isomer of ester exchange rate is more than S isomer, finally to get treated ( S) ( +) 2 - Amino propanol, yield was 97%. Whether from the economic perspective and from a practical point of view, the results are very significant, the chemical catalyst incomparable. Organic phase enzyme catalytic esterification split citalopram intermediates, antidepressant citalopram ( citalopram) 5 - is the new generation Serotonin ( 5 - HT) Reuptake inhibitors ( SSRIs) Compared with other SSRIs, for 5 - HT reuptake inhibition of strong, high selectivity. Research shows that S type is the activity of citalopram R type of more than 100 times. ( S) - 4 - ( 4 - ( Dimethyl amine) - 1 - ( 4 - Fluorinated phenyl) - 1 - The hydroxyl butyl] - 3 - ( Hydroxy methyl) Synthesis of benzyl cyanide is ( S) - Citalopram important intermediates, chiral center on the quaternary carbon connections have a tertiary alcohols, the current can be obtained by chemical method and enzymatic resolution glycol S single enantiomers, further reaction ( S) - Citalopram. Chemical method such as induced crystallization and chiral chromatographic separation is high cost, low income products optical purity, low yield issue. Compared with chemical method, the enzymatic resolution has the advantages of mild reaction condition, high selectivity, enzymatic split down the sexual medicine in terms of the preparation of enantiomerically pure compounds showed the huge development potential and broad application prospects. Lipase catalyzed selective catalytic primary alcohol and secondary alcohol has been widely used, because of the space steric effect, only a small amount of enzyme that contains quaternary carbon chiral center of tertiary alcohol selective. Studies show that from candida Antarctica ( 干地亚南极洲) And Onions pseudomonas ( 假单胞菌不过) Lipase by catalytic distance of quaternary carbon chiral center four primary hydroxyl turn esterification or chemical bond hydrolysis reaction
remote split diol, and has good selectivity.
( 2) Esterification break up down the drug
similar to the principle of separation of racemic alcohol and acid in non-aqueous enzymatic esterification process is only one enantiomer easy to participate in the reaction, so that the racemic form get split. Naproxen, ibuprofen, ibuprofen and other non-steroidal anti-inflammatory drugs in biological activities in different enantiomers have difference, confirmed s-shaped naproxen anti-inflammatory activity in the body is R type 28 times. The anti-inflammatory drugs are 2 - Aryl propionic acid ( CH3CHArCOOH) Derivatives, the optical pure naproxen, ibuprofen, etc by optical pure 2 - The preparation of aryl propionic acid. Tsai, such as use of lipase in organic solvent by selective esterification reaction by optical pure aromatic propionic acid, thus further get efficient non-steroidal anti-inflammatory drugs.
organic medium enzymatic hydrolysis reaction in the preparation of chiral drugs
in the process of some enzymes in the hydrolysis of ester, can only be applied to a single enantiomer of acetate optical active acid or alcohol, and the other a pair of the hydrolysis of ester is not enantiomers, and the product of optical pure acid or alcohol. Fat hydrolase, proteolytic enzymes and esterase is a common hydrolytic enzymes. Vantol using pig pancreatic lipase in organic solvent such as hydrolysis of 2, 3 epoxy propyl alcohol butyrate, received a single enantiomer of epoxy propyl alcohol. Epoxy propyl alcohol is a kind of beta blockers drugs synthesis intermediate. Type of propranolol S isomer can be used to treat high blood pressure and myocardial infarction, its intermediates for ( ±) - 1 - Chlorine - 3 - ( 1 - Naphthalene chloride) - 2 - Propyl alcohol, naphthalene oxygen chloride propyl alcohol. Before preparation of the despun naphthalene oxygen chloride propyl alcohol ester, reuse of lipase in organic solvent in the hydrolysis of the racemic naphthalene oxygen chloride propyl alcohol ester, got high enantiomeric value ( More than 95%) Ester of R and S ester hydrolysis acid and alcohol. Finally by the optical pure naphthalene oxygen chloride propyl alcohol preparation the s-shaped propranolol.
enzyme catalysis in the organic solvent in fine chemical, pharmaceutical and specialty in the development of the new material and agriculture has wide prospects of application of enzyme reaction in organic medium for both the enzyme, and is an attractive for chemists to new areas. A large number of experiments had been effectively prove the enzymes in organic solvents can maintain its biological activity and can be smoothly some reaction of great significance, and in organic synthesis reaction showed a good application prospect. Of enzymes in organic solvents but influence the reaction factors are complicated, the nature of the solvent, different enzymes in different solvents on the required water content requirements, the substrate properties and so on all affect the yield and selectivity of the reaction, Regioselectivity and stereoselectivity) For on enzymatic reaction in organic medium inherent law and predict remains to be the result of the reaction for a large number of experiments and deep research to get a satisfactory answer.

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