57302-79-1Relevant academic research and scientific papers
Synthesis and Antifungal Activity of β -Hydroxysulfides of 1,3-Dioxepane Series
Pavelyev, Roman S.,Vafina, Rusalia M.,Balakin, Konstantin V.,Gnezdilov, Oleg I.,Dobrynin, Aleksey B.,Lodochnikova, Olga A.,Musin, Rashid Z.,Chmutova, Galina A.,Lisovskaya, Svetlana A.,Nikitina, Liliya E.
, (2018)
Synthesis of β-hydroxysulfides of 1,3-dioxepane series and their further functionalization were performed. Chiral β-hydroxysulfides were separated into enantiomers using enzymatic acylation by lipase PS. Study of antifungal activity of the obtained compou
Influence of ester chain length, enzyme, and physical parameters on lipase-catalysed hydrolyses of meso-oxiranedimethanol esters. Part 2
Moseley, Jonathan D.,Staunton, James
, p. 3197 - 3209 (2000)
A range of meso-oxiranedimethanol diesters were prepared and subjected to hydrolysis by a selection of microbial and porcine-derived lipases. The best chain length was then subjected to a wider range of lipases. The physical reaction parameters were furth
Enzymatic resolution of syn-2-azido-1,3,4-trihydroxybutane catalysed by lipases in the transesterification mode
Iacazio,Martini,Sanchez,Faure
, p. 1313 - 1321 (2000)
The enzymatic resolution of both syn-2-azido-1,3,4-trihydroxybutane 1 and syn-2-azido-1,4-diacetoxy-3-hydroxybutane 2 have been undertaken with different lipases as catalysts and vinyl acetate as acylating agent. Lipases Amano PS and Amano AK proved to be the superior catalysts for this resolution. Indeed, both enantiomers of 1 are easily available in good yields and very good e.e.s (up to >99%). The use of chiral HPLC with a Chiralcel OD- H column allowed the determination of e.e.s of both diacetate 2 and triacetate 3 (syn-2-azido-1,3,4-triacetoxybutane) in a single analysis and thus facilitated the precise control of the reaction. (C) 2000 Elsevier Science Ltd.
Polyol synthesis through hydrocarbon oxidation: De novo synthesis of L-galactose
Covell, Dustin J.,Vermeulen, Nicolaas A.,Labenz, Nathan A.,White, M. Christina
, p. 8217 - 8220 (2008/02/09)
(Chemical Equation Presented) Carbohydrates from hydrocarbons : A hydrocarbon oxidation strategy for the synthesis of chiral polyols is validated by the enantioselective, de novo synthesis of differentially protected L-galactose (see scheme, TBS = tert-bu
N-ARYL-SUBSTITUTED CYCLIC AMINE DERIVATIVE AND MEDICINE CONTAINING THE SAME AS ACTIVE INGREDIENT
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Page 42, (2010/02/05)
The present invention provides an excellent squalene synthase inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 represents an optionally substituted vinyl group or an aromatic ring which may be substituted; ???n is an integer of 0 to 2; ???X, Y and Z are the same as or different from each other and each represents an optionally substituted carbon atom, or an optionally substituted nitrogen a tom, sulfuratomoroxygenatom, and Y optionally represents a single bond, and when Y represents the single bond, the ring to which X, Y and Z belong is a 5-membered ring; ???CyA represents a 5- to 14 membered non-aromatic cyclic amino groupornon-aromatic cyclic amidogroupwhichmaybe substituted, and the non-aromatic cyclic amino group or the non-aromatic cyclic amido group optionally having an oxygen atom or a sulfur atom; ???W represents a chain expressed by(1) optionally substituted -CH2-CH2-,(2) optionally substituted -CH=CH-,(3) -C≡C-,(4) an optionally substituted phenylene group,(5) a single bond,(6) -NH-CO-,(7) -CO-NH-,(8) -NH-CH2-,(9) -CH2-NH-,(10) -CH2-CO-,(11) -CO-CH2-,(12) -O-(CH2)m-,(13) -(CH2)m-O- (where m represents an integer of 0 to 5),(14) -O-CH2-CR2=,(15) -O-CH2-CHR2- (where R2 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom),(16) -NH-S(O)1-,(17) -S(O)1-NH-,(18) CH2-S(O)1-, or(19) -S(O)2-CH2- (where 1 represents 0, 1, or 2); and ???A represents a group having any of the following structural formulae: (wherein R3 and R4 represent independently a hydrogen atom or an optionally substituted C1-6 alkyl group, or combine through a carbon chain optionally containing a heteroatom to form a ring; ???R5 and R6 represent independently a hydrogen atom or an optionally substituted C1-6 alkyl group, or combine through a carbon chain optionally containing a heteroatom to form a ring; ???R7 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, a hydroxyl group, an alkoxy group, a halogen atom or an optionally substituted amino group; ???R8 represents a hydrogen atom, a hydroxyl group, an alkoxy group, a halogen atom or an optionally substituted amino group; ???B1 represents an optionally substituted carbon atom, or an optionallysubstitutednitrogenatom, oxygen atom or sulfur atom; ???B2 represents an optionally substituted carbon atom or nitrogen atom; ???a and b represent an integer of 0 to 4, provided that a+b is an integer of 0 to 4; ???c represents 0 or 1; and----- represents a single bond or a double bond, provided that when c is 1 in which A is a quinuclidine having R8 represented by the case where R8 is a hydrogen atom or a hydroxyl group; Arl is an aromatic heterocycle; and W is one of (1) to (3), (6) to (11) and (16) to (19) are excluded).
Effect of phosphorylation on the reaction rate of unnatural electrophiles with 2-keto-3-deoxy-6-phosphogluconate aldolase
Cotterill, Ian C.,Shelton, Michael C.,Machemer, Daniel E. W.,Henderson, Darla P.,Toone, Eric J.
, p. 1335 - 1341 (2007/10/03)
D-Glyceraldehyde is accepted as an electrophile by 2-keto-3-deoxy-6-phosphogluconate (KDPG) aldolase (EC 4.1.2.14) at 1% the rate of natural substrate, D-glyceraldehyde 3-phosphate. Accordingly, it was expected that addition of a phosphate moiety at C3 or C4 of unnatural aldehydes would enhance their activity as electrophilic substrates. Furthermore, phosphate would act as a useful protecting group during synthetic manipulations of the aldol adduct. A variety of phosphorylated and non-phosphorylated aldehydes were synthesized and evaluated as substrates for KDPG aldolase. Although small variations in reaction rate were observed, phosphorylation failed to provide a universal rate enhancement. Evaluation of substrate kinetic parameters revealed that the high rate of reaction of D-glyceraldehyde 3-phosphate compared to related electrophiles is entirely due to the efficiency of turnover with little change in binding exhibited among various substrates.
Selective epoxidations involving anionic peroxotungsten compounds generated in situ on layered double hydroxides with various polarities
Sels, Bert F.,De Vos, Dirk E.,Jacobs, Pierre A.
, p. 8557 - 8560 (2007/10/03)
WO42-exchanged LDH catalyses the epoxidation of simple olefins and allylic alcohols. Substrate reactivity, chemo- and regioselectivity vary markedly with the polarity of the peroxotungstate environment.
Process for forming omega-deuxy-azasugars
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, (2008/06/13)
A process for the preparation of a 1,5-dideoxyazafuranose or 1,6-dideoxy-azapyranose is disclosed. In such a process, an azido-substituted α-ketose phosphate having a five- or a six-carbon chain is hydrogenated in the presence of a palladium catalyst. The carbon atom bearing the azido substituent and the carbon atom of the keto group of the α-ketose phosphate starting material are separated by two or three carbon atoms.
2-methyl-5-hydroxymethyl- and 2,5-dimethyl-3,4-dihydroxypyrrolidines
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, (2008/06/13)
2-Methyl-5-hydroxymethyl- and 2,5-dimethyl-3,4-dihydroxypyrrolidines, 2,5-dimethyl-3,4-dihydroxypyrrolidines, their processes of preparation and use are disclosed. 5-Azido-5-deoxyhexulose-1-phosphate compounds and processes of making the same are also disclosed.
Synthesis of optically pure cis epoxyalcohols via an enzymatic route; an alternative to the sharpless asymmetric epoxidation
Grandjean,Pale,Chuche
, p. 3043 - 3046 (2007/10/02)
Optically pure (2S, 3R)-4-butyryloxy-2,3-epoxybutan-1-ol 2b and (2R, 3S)-4-tert-butyldiphenylsilyloxy-2,3-epoxybutan-1-ol 5, starting materials for the synthesis of enantiomeric epoxyalcohols 3 and 4, were obtained after enzymatic hydrolysis of meso cis-2,3-epoxybutane-1,4-diol diesters 1b.
