609-12-1Relevant academic research and scientific papers
Synthesis of α-alkylated γ-butyrolactones with concomitant anhydride kinetic resolution using a sulfamide-based catalyst
Claveau, Romain,Twamley, Brendan,Connon, Stephen J.
supporting information, p. 7574 - 7578 (2018/11/02)
The Kinetic Resolution (KR) of α-alkylated enolisable disubstituted anhydrides has been shown to be possible for the first time. In the presence of an ad hoc designed novel class of bifunctional sulfamide organocatalyst, a regio-, diastereo- and enantioselective cycloaddition reaction between the enolisable anhydride and benzaldehydes provides densely functionalised γ-butyrolactones in one pot (up to 19:1 dr, 94% ee) with control over three contiguous stereocentres. The concomitant resolution of the starting material anhydride, provides access to a range of chiral succinate derivatives with selectivity factors up to S? = 10.5.
CARBAZOLE DERIVATIVE, SOLVATE THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Page/Page column 42, (2010/11/28)
An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like. The above-mentioned object can be achieved by carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof, wherein the carbazole derivatives are represented by the following general formula (I): (In the formula (I), the ring A represents phenyl group or the like; X represents -O- or the like; Y represents =N- or the like; a and b represent methylene group or the like; both V and Z represent -O- or the like; W represents a C1-C10 alkylene group whose 1 or 2 hydrogen atoms may be substituted by a phenyl group or a C1-C6 alkyl group; 1,2-phenylene group; 1,3-cyclohexyl group; or the like; R1 represents methyl group or the like; R2 represents methoxy group or the like; and R3 represents carboxy group or the like.)
Pyrimidine acyclonucleoside derivatives, preparation method and use thereof
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Page/Page column 15-16, (2010/02/12)
The invention relates to a compound having general formula (I): wherein n is equal to 3; R1 is an ethyl or isopropyl group; each of the R2 groups is independently of each other a hydrogen atom, a C1-C3 alkyl group or a halogen atom; one of the R3 and R4 groups represents a hydrogen atom while the other of the R3 and R4 groups represents an OH or OR5 group, where R5 can be a C2-C7 acyl group, an alkyl(C1-C6)animo-carbonyl group, an aralkyl(C1-C6)aminocarbonyl optionally substituted on the aryl, an arylcarbonyl group optionally substituted or a heteroarylaminocarbonyl group. Said compound is particularly suitable as an antiviral agent and especially as an anti-HIV-1 agent.
Syntheses based on monocarbon molecules: II. Synthesis of ethyl isovalerate by isobutene carbonylation with carbon monoxide and ethanol in the presence of phosphine palladium complexes. Ethyl α-bromoisovalerate
Suerbaev,Abyzbekova,Shalmagambetov,Zhubanov
, p. 516 - 517 (2007/10/03)
Optimal conditions for the synthesis of ethyl isovalerate by isobutene hydrocarbalkoxylation with carbon monoxide and ethanol in the presence of the catalytic system PdCl2(PPh3)2 + PPh3 + p-TsOH were found. Bromination of ethyl isovalerate under conditions of the Hell-Volgard-Zelinskii reaction gave ethyl α-bromoisovalerate which is the main active component in korvalol medicine.
Direct gaschromatographic separation of drug racemates
Schleuder,Duerrbeck,Jira
, p. 381 - 386 (2007/10/03)
For inspection of the direct separability of synthetic drug racemates through GC/MS a uniform scheme is proposed and checked with 35 drugs and two cyclodextrin capillary columns. All investigated analytes vaporized without decomposition, 26 of them are separable in the enantiomers, among them 10 with separation to the baseline and 14 with CO-NH-structure.
The Development of Cyclic Sulfolanes as Novel and High-Affinity P2 Ligands for HIV-1 Protease Inhibitors
Ghosh, Arun K.,Lee, Hee Yoon,Thompson, Wayne J.,Culberson, Chris,Holloway, M. Katharine,et al.
, p. 1177 - 1188 (2007/10/02)
Design and synthesis of a novel series of protease inhibitors incorporating conformationally constrained cyclic ligands for the S2-substrate binding site of HIV-1 protease is described. We recently reported urethanes of 3-tetrahydrofuranyl as P2 ligands for HIV-1 protease inhibitors. Subsequently, we have found that the urethane of 3(S)-hydroxysulfolane further increased the in vitro potency of these inhibitors. Furthermore, introduction of a small 2-alkyl group cis to the 3-hydroxyl group of either heterocyclic system further enhanced enzyme affinity. The cis-2-isopropyl group thus far offered optimum enhancement of the inhibitory properties. This led to the discovery of inhibitor 43 (IC50 3.5 nM, CIC95 50+/-14 nM) of comparable in vitro antiviral potency to the current clinical candidate 1 (Ro 31-8959) but of reduced molecular weight due to the exclusion of the P3 quinoline ligand. Also, it has been demonstrated that the octahydropyrindene derivative 34 is an effective replacement of the P1' decahydroisoquinoline derivative.
Preparation of substituted alpha-halogeno-propionic acids and their derivatives
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, (2008/06/13)
Substituted α-halogenopropionic acids and their derivatives of the general formula STR1 wherein R1 to R3, Y and X have the meanings given in the description, are prepared by a process which is characterized in that substituted vinylidene chlorides of the general formula STR2 are reacted with chlorine or bromine chloride in the presence of compounds of the formula wherein R5 and R6 have the meaning given in the description, and the products obtained are treated, if appropriate, with water or alcohol. Certain of the substituted α-halogeno-propionic acids and the substituted vinylidene chloride of the formula STR3 are new. The end products are useful as herbicides and intermediates for insecticides.
Unnatural nucleosides and nucleotides. III. Preparation of 2-14C and 4-14C labelled 5-alkyluracils and 5-alkyl-2'-deoxyuridines
Szabolcs,Kruppa,Sagi,Otvos
, p. 713 - 726 (2007/10/08)
2-14C Labelled 5-alkyluracils were prepared by condensation of the diethylacetals of α-formyl-carbonic acid esters with 14C-thiourea. Compounds labelled at 4-C were synthesized by condensation of the labelled carboxylic acid derivatives with thiourea. β-Anomers of 5-alkyl-2'-deoxyuridines were obtained in a fairly good radiochemical yield. Alkyl substituents ranged from methyl to tetradecyl, isopropyl and tert-butyl.
