- Method and device for continuously producing thiopropionate series compounds through pipeline type
-
The invention discloses a method and a device for continuously producing thiopropionate series compounds through pipeline type, and can simultaneously or separately prepare thiodipropionate compounds. Dithionate type compounds and mercapto ester compounds. The method is simple to operate, low in cost and high in yield, and is suitable for industrial production.
- -
-
Paragraph 0100-0101; 0106-0109; 0110-0111
(2021/11/27)
-
- Optimization of 1,2,3,4-tetrahydroacridin-9(10 H)-ones as antimalarials utilizing structure-activity and structure-property relationships
-
Antimalarial activity of 1,2,3,4-tetrahydroacridin-9(10H)-ones (THAs) has been known since the 1940s and has garnered more attention with the development of the acridinedione floxacrine (1) in the 1970s and analogues thereof such as WR 243251 (2a) in the 1990s. These compounds failed just prior to clinical development because of suboptimal activity, poor solubility, and rapid induction of parasite resistance. Moreover, detailed structure-activity relationship (SAR) studies of the THA core scaffold were lacking and SPR studies were nonexistent. To improve upon initial findings, several series of 1,2,3,4-tetrahydroacridin-9(10H)-ones were synthesized and tested in a systematic fashion, examining each compound for antimalarial activity, solubility, and permeability. Furthermore, a select set of compounds was chosen for microsomal stability testing to identify physicochemical liabilities of the THA scaffold. Several potent compounds (EC50 100 nM) were identified to be active against the clinically relevant isolates W2 and TM90-C2B while possessing good physicochemical properties and little to no cross-resistance.
- Cross, R. Matthew,Maignan, Jordany R.,Mutka, Tina S.,Luong, Lisa,Sargent, Justin,Kyle, Dennis E.,Manetsch, Roman
-
experimental part
p. 4399 - 4426
(2011/09/15)
-
- An improved and green preparation of 3-(alkylthio)propionic acids
-
An efficient, facile microwave-assisted synthesis has been developed for the preparation of unsymmetrical sulfide derivatives from 3-mercaptopropionic acid and a wide variety of alkyl, allyl or aryl chlorides or bromides. The synthesis performed in ethanol at 80 or 120 °C using sodium hydroxide as a base, selectively without an offensive smell, generates 3-(alkylthio)propionic acids in good yields. Effects of reaction components, temperature, and the heating technique on the formation of the product and side-products were studied.
- Vaismaa, Matti J. P.,Yliniemel?, Sanna M.,Lajunen, Marja K.
-
p. 1317 - 1323
(2008/10/09)
-
- Tributylphosphine, excellent organocatalyst for conjugate additions of non-nucleophilic N-containing compounds
-
Conjugate additions of non-nucleophilic N-containing compounds such as amides, thioamides, sulfonamides, and electron-poor anilines with different Michael acceptors can be promoted through the use of tributylphosphine. The range of useful pKa's of nucleophiles has been established (pKa25) and new insights into the mechanism proposed.
- Gimbert, Carolina,Moreno-Ma?as, Marcial,Pérez, Elisabet,Vallribera, Adelina
-
p. 8305 - 8310
(2008/02/05)
-
- High regioselectivity in the heterocyclization of β-oxonitriles to 4-oxothiazolidines: X-ray structure proof
-
Base-catalyzed reactions of β-oxonitriles 1 with diethyl mercaptosuccinate favour heterocyclization to afford 2-alkylidene-4-oxothiazolidines 3, rather than 2-alkylidene-4-oxo-1,3-thiazinanes 4. The observed regioselectivity is based on spectroscopic and experimental evidence, including a single-crystal X-ray structure determination.
- Markovi?, Rade,Baranac, Marija,D?ambaski, Zdravko,Stojanovi?, Milovan,Steel, Peter J.
-
p. 7803 - 7810
(2007/10/03)
-
- Eight-membered thiocycloether via indium-mediated ring enlargement
-
The ring expansion of a thiocycloether is studied. Ethyl-4-oxo- thiotetrahydropyran-3-carboxylate was expanded to an eight-membered thiocyclo ether by using indium mediated carbon-carbon bond formation in aqueous medium.
- Li, Chao-Jun,Chen, Dong-Li
-
p. 735 - 736
(2007/10/03)
-
- N-Ethyldiisopropylamine and Sulfur Dioxide Solutions. 2. Reactions with Conjugate Acceptors
-
Solutions of sulfur dioxide and N-ethyldiisopropylamine (EDIA) are able to reduce α,β-unsaturated-γ-dicarbonyl compounds (esters or ketones) into α-dicarbonyl alkanes.In contrast, monoactivated Michael acceptors, such as acrylates, give symmetrical sulfones.These processes involve the conjugate addition of HSO2(-), formed from a charge-transfer complex between EDIA and SO2.Secondary amines are formed as byproducts.Triethylamine, which forms a more stable complex with sulfur dioxide than EDIA, is far less reactive toward the same substrates.
- Eugene, Fabrice,Langlois, Bernard,Laurent, Eliane
-
p. 2599 - 2603
(2007/10/02)
-
- REDUCTION AND SULFONYLATION OF OLEFINS BY SOLUTIONS OF DIISOPROPYLETHYLAMINE AND SULFUR DIOXIDE
-
Solutions of diisopropylethylamine and SO2 deliver sulfones from acrylates and reduce olefins substituted by two carbonyl moieties in α and β positions.
- Eugene, Fabrice,Langlois, Bernard,Laurent, Eliane
-
p. 377 - 378
(2007/10/02)
-
- Esters of Thiodiglycollic and Thiodipropionic Acids and 2,5-Dicarboxy-3,4-dihydroxythiophene as Potential Slow Acting Anticancer Agents
-
A series of esters of thiodiglycollic and thiodipropionic acids and 2,5-dicarboxy-3,4-dihydroxythiophene have been synthesised with a view to testing their anticancer properties.The esters, as against parent acids are expected to have a prolonged effect.
- Kumar, Anil,Tilak, B. D.
-
p. 880 - 882
(2007/10/02)
-
