- Implementation of biocatalysis in continuous flow for the synthesis of small cyclic amines
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Significant progress has been made in establishing transaminases as robust biocatalysts for the green and scalable synthesis of a diverse range of chiral amines.[1] However, very few examples on the amination of small cyclic ketones have been reported.[2] Cyclic ketones are particularly challenging for transaminase enzymes because they do not display the well-defined small and large substituent areas that are characteristic for the biocatalytic mechanism. In this work, we exploited the broad substrate scope of the (S)-selective transaminase from Halomonas elongata (HeWT) to develop an efficient biocatalytic system in continuous flow to generate a range of small cyclic amines which feature very often in pharmaceuticals and agrochemicals.[3] Tetrahydrofuran-3-one and other challenging prochiral ketones were rapidly (5-45 min) transformed to their corresponding amines with excellent molar conversion (94-99%) and moderate to excellent ee.
- Hegarty, Eimear,Paradisi, Francesca
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p. 890 - 894
(2020/12/25)
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- Widely applicable background depletion step enables transaminase evolution through solid-phase screening
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Directed evolution of transaminases is a widespread technique in the development of highly sought-after biocatalysts for industrial applications. This process, however, is challenged by the limited availability of effective high-throughput protocols to evaluate mutant libraries. Here we report a rapid, reliable, and widely applicable background depletion method for solid-phase screening of transaminase variants, which was successfully applied to a transaminase from Halomonas elongata (HEWT), evolved through rounds of random mutagenesis towards a series of diverse prochiral ketones. This approach enabled the identification of transaminase variants in viable cells with significantly improved activity towards para-substituted acetophenones (up to 60-fold), as well as tetrahydrothiophen-3-one and related substrates. Rationalisation of the mutants was assisted by determination of the high-resolution wild-type HEWT crystal structure presented herein.
- Planchestainer, Matteo,Hegarty, Eimear,Heckmann, Christian M.,Gourlay, Louise J.,Paradisi, Francesca
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p. 5952 - 5958
(2019/06/19)
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- Preparation method of (R)-tetrahydrofuran-3-amine
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The invention provides a preparation method of (R)-tetrahydrofuran-3-amine. The target product is obtained by conducting two steps of reactions including amidation and Hofmann degradation with (R)-tetrahydrofuran-3-formic acid as main materials. By means of the method, production and operation are easy, the production cycle is short, the product yield is high, no racemate is generated in the production process, the product quality is stable, cost is low, and the method is suitable for industrialized production.
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Paragraph 0023
(2017/01/19)
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- Catalytic asymmetric hydrogenation of heterocyclic ketone-derived hydrazones, pronounced solvent effect on the inversion of configuration
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An enantioselective hydrogenation of hydrazones derived from heterocyclic ketones was developed with up to 85% ee. The enantiomeric purity was enriched to >99% ee by crystallization from EtOAc in >80% yield. Optimization studies have revealed a notable so
- Haddad, Nizar,Qu, Bo,Rodriguez, Sonia,Van Der Veen, Lars,Reeves, Diana C.,Gonnella, Nina C.,Lee, Heewon,Grinberg, Nelu,Ma, Shengli,Krishnamurthy, Dhileepkumar,Wunberg, Tobias,Senanayake, Chris H.
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supporting information; experimental part
p. 3718 - 3722
(2011/08/06)
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- PURINE DERIVATIVES FOR USE IN THE TREATMENT OF ALLERGIC, INFLAMMATORY AND INFECTIOUS DISEASES
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Compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
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Page/Page column 48-49
(2010/04/03)
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- Partial and full agonists of A1 adenosine receptors
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Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, myocardial infarction and hyperlipidemia.
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- Method of treating arrhythmias
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A method for treating arrhythmias is provided comprising administering a low dose of an adenosine receptor agonist, in particular CVT-510, to a mammal in need of such treatment.
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- Pyrimido?5,4-D!pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
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The present invention relates to pyrimido?5,4-d!pyrimidines of the general formula STR1 in which Ra to Rc are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.
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- N6 mono heterocyclic substituted adenosine derivatives
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A substituted N 6 -oxa, thia, thioxa and azacycloalkyl substituted adenosine derivative and a method for using the composition as an A 1 heart adenosine receptor.
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