- Preparation methods of tiopronin and zinc complex of tiopronin
-
The invention discloses preparation methods of tiopronin and zinc complex of tiopronin and belongs to the technical field of a medicine compound for relieving acute/chronic liver diseases. The technical scheme is characterized in that the formula is shown in the specification. The operation is simple, the cost of raw materials is low, the repeatability of experimental results of a process route is higher, and the production cost can be remarkably reduced.
- -
-
Paragraph 0032; 0033; 0034; 0035
(2017/02/24)
-
- Asymmetric michael addition of substituted rhodanines to α,β-unsaturated ketones catalyzed by bulky primary amines
-
A bulky group was introduced by design into a diamine catalyst, and a series of robust and tunable bulky chiral primary amine catalysts were developed and successfully applied in the direct conjugate addition of substituted rhodanines to α,β-unsaturated ketones. High yields (up to 99%) and excellent diastereoselectivities (up to 99:1 dr) and enantioselectivities (up to 98% ee) were observed.
- Yu, Feng,Hu, Haoxiang,Gu, Xiaodong,Ye, Jinxing
-
supporting information; scheme or table
p. 2038 - 2041
(2012/07/28)
-
- Interactions between Penicillin-Binding Proteins (PBPs) and Two Novel Classes of PBP Inhibitors, Arylalkylidene Rhodanines and Arylalkylidene Iminothiazolidin-4-ones
-
Several non-β-lactam compounds were active against various gram-positive and gram-negative bacterial strains. The MICs of arylalkylidene rhodanines and arylalkylidene iminothiazolidin-4-ones were lower than those of ampicillin and cefotaxime for methicillin-resistant Staphylococcus aureus MI339 and vancomycin-resistant Enterococcus faecium EF12. Several compounds were found to inhibit the cell wall synthesis of S. aureus and the last two steps of peptidoglycan biosynthesis catalyzed by ether-treated cells of Escherichia coli or cell wall membrane preparations of Bacillus megaterium. The effects of the arylalkylidene rhodanines and arylalkylidene iminothiazolidin-4-one derivatives on E. coli PBP 3 and PBP 5, Streptococcus pneumoniae PBP 2xS (PBP 2x from a penicillin-sensitive strain) and PBP 2xR (PBP 2x from a penicillin-resistant strain), low-affinity PBP 2a of S. aureus, and the Actinomadura sp. strain R39 and Streptomyces sp. strain R61 DD-peptidases were studied. Some of the compounds exhibited inhibitory activities in the 10 to 100 μM concentration range. The inhibition of PBP 2xS by several of them appeared to be noncompetitive. The dissociation constant for the best inhibitor (Ki = 10 μM) was not influenced by the presence of the substrate.
- Zervosen, Astrid,Lu, Wei-Ping,Chen, Zhouliang,White, Ronald E.,Demuth Jr., Thomas P.,Frere, Jean-Marie
-
p. 961 - 969
(2007/10/03)
-
- Compositions containing a liquid medium and an azo dye
-
A composition comprising: (a) a liquid medium comprising (i), (ii) or (iii): (i) a mixture of water and an organic solvent; (ii) an organic solvent free from water; or (iii) a low melting point solid; and (b) a dye of the Formula (1) or a salt thereof: ?wherein A, B, Z, L, R1and n are as defined in the description. Also claimed are certain dyes of Formula (1), inks, an ink jet printing process using the inks, a substrate printed with the inks, an ink jet printer cartridge containing the inks and an ink jet printer containing the ink jet printer cartridge.
- -
-
-
- S-4-Methoxytrityl mercapto acids: Synthesis and application
-
4-Methoxytrityl (Mmt)-mercapto acids were obtained either by the reaction of mercapto acids with Mmt-chloride or by the reaction of halo acids with Mmt-thiol. The derivatives obtained were used in the solid-phase synthesis of small libraries of mercaptoacylamino acids and mercaptoacyl peptides. The removal of the Mmt-group was performed by treatment with trifluoroacetic acid (TFA) in dichloromethane (DCM) using triethylsilane (TES) as scavenger.
- Mourtas, Spyros,Gatos, Dimitrios,Kalaitzi, Vagiani,Katakalou, Christina,Barlos, Kleomenis
-
p. 6965 - 6967
(2007/10/03)
-
- Effect of the α-methyl substituent on chemoselectivity in esterase-catalyzed hydrolysis of S-acetyl sulfanylalkanoates
-
(Equation Presented) The isomeric compounds 1 and 3, which differ only in the position of a methyl substituent, give opposite chemoselectivities in an esterase-catalyzed hydrolysis reaction. The esterase was chemoselective for the oxoester in 1, but for the thiol ester group in 3. A high enantioselectivity was observed for both 1 and 3.
- Kumar, Ish,Jolly, Ravinder S.
-
p. 207 - 209
(2008/02/11)
-
- Structure-Activity Relations. Part 6. The Alkaline Hydrolysis of 3-Methyl-5-methylidene- and 3,5-Dimethylthiazolidine-2,4-diones. The Addition of Thiols to 3-Methyl-5-methylidenethiazolidine-2,4-dione
-
The rate-coefficients for the alkaline hydrolysis of 3-methyl-5-methylidene- and 3,5-dimethylthiazolidine-2,4-diones in water at 25.0 deg C have been measured.The reaction of the 5-methylidene substrat is first order in both substrate and hydroxide ion.The reaction of the 5-methyl substrate is two phase.The first and more rapid reaction of this substrat is 1.4 times faster than the only observed reaction of the former substrate.The second reaction is the hydrolysis of an intermediate, which is first order in substrate and has two components, one first and the other second order in hydroxide ion.The rate coefficient for the addition of aseries of thiols to the 5-methylidene substrate in water at pH 7.40 have been measured.A Broensted coefficient of ca. 0.37 has been found.The detailed reaction pathway and relation to Marcus and related theories are discussed.
- Bowden, Keith,Chana, Ravinder S.
-
p. 2163 - 2166
(2007/10/02)
-
- Organotin-containing composition for the stabilization of polymers of vinyl chloride
-
An organotin-containing composition for the stabilization of polymers or copolymers of vinyl chloride in which there is incorporated a stabilizing amount of an organotin compound containing at least two tin atoms and which is a mercapto, hydroxy or alkoxy substituted ester of a mercapto acid substituted organotin mercapto acid diester.
- -
-
-
- Substituted phenylguanidines and method
-
Phenylguanidine derivatives are provided having the structure STR1 wherein R1 is lower alkyl, cycloalkylalkyl, or phenylalkyl; R2 is lower alkyl, phenyl or benzyl; and R3 is lower alkyl, cycloalkylalkyl, lower alkenylalkyl, dihalovinylalkyl, dihalobutadienyl or phenylalkyl; and n is 1 to 5. These compounds are useful as anthelmintic agents.
- -
-
-
- Methods and intermediates for preparing cis-4-oxoazetidine intermediates
-
The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
- -
-
-
- Cis-4-oxoazetidine intermediates and methods of preparing them
-
The stereospecific cycloaddition of nitrogen containing acetic acid halides or anhydrides with Schiff bases having a carbalkoxy group substituted on the methine carbon atom offers new intermediates and methods for preparing synthetic cephalosporin congeners having antibacterial activity.
- -
-
-
- 8-Oxo-4-thia-1-azabicyclo (4.2.0)-oct-2-ene derivatives
-
Novel bicyclic β-lactams and intermediates useful in their preparation are disclosed. In particular, 7β-acyl-amino- and 7β-amino-8-oxo-4-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acids are prepared. The acylated compounds are antibacterial agents.
- -
-
-
- Azole derivatives
-
Azole derivatives of the formula SPC1 Wherein R1 is free or esterified carboxyl or other functionally modified carboxyl group, R2 and R3 each are aryl; A is Cn H2n in which n is an integer from 1 to 10, inclusive; and Z is O or S; and the physiologically acceptable salts thereof, possess, with good compatibility, excellent antiphlogistic activity and, in particular, influence favorably the chronic progressive diseases of the joints, e.g., arthritis. They can be prepared from compounds of the formula SPC2 Wherein X1 is a group convertible into the group --S--A--R1, and R2 and R3 have the values given above.
- -
-
-
