- A metagenomics approach for new biocatalyst discovery: Application to transaminases and the synthesis of allylic amines
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Transaminase enzymes have significant potential for the sustainable synthesis of amines using mild aqueous reaction conditions. Here a metagenomics mining strategy has been used for new transaminase enzyme discovery. Starting from oral cavity microbiome samples, DNA sequencing and bioinformatics analyses were performed. Subsequent in silico mining of a library of contiguous reads built from the sequencing data identified 11 putative Class III transaminases which were cloned and overexpressed. Several screening protocols were used and three enzymes selected of interest due to activities towards substrates covering a wide structural diversity. Transamination of functionalized cinnamaldehydes was then investigated for the production of valuable amine building blocks.
- Baud, Damien,Jeffries, Jack W. E.,Moody, Thomas S.,Ward, John M.,Hailes, Helen C.
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p. 1134 - 1143
(2017/08/14)
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- COMPOSITIONS AND METHODS USING THE SAME FOR TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE
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The present disclosure is directed, in part, to compounds, or pharmaceutically acceptable salts thereof, for the treatment and/or prevention of neurodegenerative disease and/or mitchonodrial disease including Parkinson's disease and Leigh's disease.
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Page/Page column 120
(2015/09/22)
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- Modular synthesis of 1,2-Diamine derivatives by palladium-Catalyzed aerobic oxidative cyclization of allylic sulfamides
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Chemical equation presented Allylic sulfamides undergo aerobic oxidative cyclization at room temperature, mediated by a Pd(O 2CCF3)2/DMSO catalyst system in tetrahydrofuran. The cyclic sulfamide products are readily converted into 1,2-diamines, and substrates derived from chiral allylic amines cyclize with very high diastereoselectivity.
- McDonald, Richard I.,Stahl, Shannon S.
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supporting information; experimental part
p. 5529 - 5532
(2010/09/05)
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- Rhodium(I)-catalyzed ene-allene carbocyclization strategy for the formation of azepines and oxepines
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A novel strategy for the preparation of seven-membered heterocyclic compounds has been realized. Treatment of ene-allene 1 with a catalytic quantity of rhodium biscarbonyl chloride dimer affords the cyclization product 2 in moderate to high yields. The sc
- Brummond, Kay M.,Chen, Hongfeng,Mitasev, Branko,Casarez, Anthony D.
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p. 2161 - 2163
(2007/10/03)
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- Synthesis of 2,3-disubstituted pyrroles from 3,N-dilithio-N-(tert-butyldimethylsilyl)-2-buten-1-amine
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N-(Trialkylsilyl)allylamines can be deprotonated at the cis-vinylic position to yield 3,N-dilithio-N-(trialkylsilyl)allylamines under mild conditions. N-(Trialkylsilyl)allylamines with terminal alkyl substituents were reported not to form dianions under t
- Jacobson, Madeleine A.,Williard, Paul G.
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- Thermolysis of N-Allylic 1,2,4-Triazoles
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A number of 4-allylic substituted 3,5-diphenyl-4H-1,2,4-triazoles were thennolyzed at 315-320° in evacuated glass ampoules. The main reaction in the melt was rearrangement to the corresponding 1-substituted triazoles, which appeared to proceed via competing SN2 and SN2′ mechanisms. The allylic systems were observed to undergo [2,3]-allyl walk reactions between the 1- and 2-ring positions. Allyl to vinyl isomerization also took place. Substitution of the allylic moiety increased the rate of reaction but decreased the rate of isomerization of allylic to the vinylic substituted triazoles. The 4-vinyl substituted triazoles were inert under the reaction conditions. Some triazoles were converted into substituted pyridines. This was proposed to proceed via nitrogen extrusion and formation of a 1,3-dipolar intermediate (nitrile ylide) which added intramolecularly to the allyl moiety and subsequently aromatized to the pyridine.
- Carlsen, Per H. J.,Jorgensen, Kare B.
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p. 797 - 806
(2007/10/03)
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- Synthesis of primary amines using potassium 1,1,3,3-tetramethyldisilazide as aminating agent of alkyl halides
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A one-pot synthesis of various primary amines is described. Potassium 1,1,3,3-tetramethyldisilazide, prepared from 1,1,3,3-tetramethyldisilazane and potassium hydride, reacts with alkyl bromides, iodides, tosylates, benzylic chlorides, and allylic chlorides to give the corresponding N,N-bis(dimethylsilyl)amines in high yields. Subsequent deprotection of the dimethylsilyl group was performed under mildly acidic conditions to afford primary amines. This method was also applied to the preparation of aminomethylated cross-linked polystyrene.
- Itsuno,Koizumi,Okumura,Ito
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p. 150 - 152
(2007/10/02)
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- Derivatives of leukotrienes A and C
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The present invention provides novel derivatives of leukotrienes A and C which are useful in inhibiting the smooth muscle contracting effects of SRS-A; inhibiting platelet aggregation; and inhibiting the biosynthesis of thromboxane A2.
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- The Reactions of Singlet NH Radicals with C4 Olefins in the Liquid Phase
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The reactions of NH radicals with C4 olefins, trans- and cis-2-butenes, 1-butene, and isobutene, were investigated by the photolysis of hydrogen azide in the liquid olefin at 0 deg C and at the temperature of Dry Ice-methanol.Except for nitrogen and ammonia, amines and aziridines were found to be formed in good yield. 2-Butene-1-amine and trans-2,3-dimethylaziridine from trans-2-butene, 2-butene-1-amine and cis-2,3-dimethylaziridine from cis-2-butene, 3-butene-1- and 2-amines and 2-ethylaziridine from 1-butene, and 2-methyl-2-propene-1-amine and 2,2-dimethylaziridine from isobutene.These product formations were successfully explained by the insertion into the C-H bond and the addition to the double bond of olefin by the singlet NH radicals.In the case of 2-butene, no isomerized aziridine formation was observed.This result suggested that the triplet NH radicals rarely add to the double bond of olefin.
- Hamada, Jun-ichi,Tsunashima, Shigeru,Sato, Shin
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p. 662 - 666
(2007/10/02)
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- 19-Hydroxy-PGI2 compounds
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Prostacyclin and prostacyclin-type derivatives having a 19-hydroxy feature are disclosed, including processes for preparing them and the appropriate intermediates. The compounds are useful for pharmacological purposes such as inhibition of blood platelate aggregation.
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- 2-Decarboxy-2-hydroxymethyl-19-hydroxy-PG1 analogs
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Prostaglandin derivatives having a 19,20-didehydro, a 19-hydroxy, or a 19-keto feature are disclosed, including processes for preparing them and the appropriate intermediates. A typical 19-hydroxy compound of this invention is 19-hydroxy-19-methyl-PGF2α, methyl ester, represented by the formula STR1
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- Production of primary and secondary amines by reaction of ammonia with conjugated diene in the presence of Pd/phosphine catalyst and primary or secondary aliphatic alcohol solvent medium
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Short chain, unsaturated primary and secondary amines are prepared by reaction of ammonia and conjugated dienes in a primary or secondary aliphatic alcohol solvent medium and in the presence of a catalyst system comprising a palladium compound co-catalyzed with a phosphine ligand containing 2 to 4 phosphorus atoms.
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- Process for converting esters to amine salts
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A new method for converting certain diesters to physiologically acceptable amines which comprises reacting the diester with the desired amine in a solvent consisting essentially of water.
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- Pharmaceutical compositions and methods of inhibiting gastric acid secretion
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Pharmaceutical compositions and methods of inhibiting gastric acid secretion by administering N-alkenyl and N-alkynyl thioamides.
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- 2-Alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides
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The compounds are 2-alkoxy(and 2-amino)-3-amino-2-heterocyclic-thiopropanamides, for example 2-methoxy-N-methyl-3-morpholino-2-(2-pyridyl)thiopropanamide, which are inhibitors of gastric acid secretion.
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