104527-63-1

Upstream product

• 108-24-7 acetic anhydride 
• 34592-47-7 L-thioproline 
• 33898-90-7 2-Thenoylacetonitrile 
• 50-00-0 formaldehyd 
• 207121-46-8 D‐cysteine hydrochloride monohydrate 
• 444-27-9 (RS)-4-thiazolidinecarboxylic acid 

Relevant academic research and scientific papers

Synthetic method for efficiently preparing folcisteine

The invention discloses a synthetic method for efficiently preparing folcisteine, belonging to the field of organic chemistry, comprising the following reaction steps: S1: reacting L-cysteine and 37%aqueous formaldehyde solution until L-cysteine is fully reacted to obtain L-thioproline; S2: directly adding an acetylation reagent to the system obtained by S1, and performing one-pot reaction untilL-thioproline is completely reacted; S3: adjusting the pH of the system obtained by S2 to 5-6, adding activated carbon for heating and decolorizing, cooling, adjusting the pH to 1-3, cooling and crystallizing to obtain folcisteine. The one-pot reaction is adopted for preparing acetyl thioproline, to avoid the post-treatment step of extracting intermediate thioproline after the first step reaction,shorten the process route, reduce the operation steps, and improve the work efficiency.

Synthetic method for timonacic pharmaceutical intermediate--L-N-acetyl thioproline

The invention provides a synthetic method for a timonacic pharmaceutical intermediate--L-N-acetyl thioproline. The synthetic method comprises the following steps: (I) adding 0.11 mol of L-thioproline and 80 to 100 ml of a potassium chloride solution into a reaction vessel, controlling a stirring speed in a range of 100 to 150 rpm, heating the mixed solution to 80 to 85 DEG C, slowly dropwise adding 50 ml of 2-thiopheneacetylnitrile and controlling addition time in a range of 30 to 40 min, keeping the stirring speed in a range of 90 to 120 min, carrying out reduced pressure distillation until a solid is precipitated, adding 80 ml of p-xylene, carrying out heating and redissolving the solid, carrying out decolorizing by using a molecular sieve, keeping a solution temperature in a range of 10 to 15 DEG C, carrying out standing for 30 to 35min, filtering a solid, and carrying out dehydrating by using a dehydrating agent so as to obtain white L-N-acetyl thioproline (1), wherein the mass fraction of the potassium chloride solution in the step (I) is 10 to 15%, and the mass fraction of 2-thiopheneacetylnitrile in the step (I) is 70 to 85%.

Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads

The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.

Synthesis and biological evaluation of new naphthoquinone-containing pyrrolo-thiazoles as anticancer agents

(Chemical Equation Presented) Naphthoquinones undergo 1,3-dipolar cycloaddition with bicyclic muenchnones generated from thiazolidines affording new pyrrolo-thiazoles with a fused quinone nucleus. The products were obtained as single enantiomers in good yields. These benzo[f]thiazolo[4,3-a] isoindole-6,11(1H,3H)-diones are comprised of four fused rings and present a very planar structure. The evaluation of their anticancer activity against melanoma A375 and colorectal adenocarcinoma WiDr human cell lines showed only moderate activity but gave insight into the modeling of new structures. [Color figure can be viewed in the online issue, which is available at www.interscience.wiley.com.]

PROCESS FOR OBTAINING MIXTURES OF 4-CARBOXY-1,3-THIAZOLIDINIUM CARBOXYLATE AND N-ACYL-1,3-THIAZOLIDIN-4-CARBOXYLIC ACID

The present invention relates to a process for obtaining in a single synthesis stage mixtures of 4-carboxy-1,3-thiazolidium carboxylate and N-acyl-1, 3-thiazolidin-4- carboxylic acids from 1,3-thiazolidin-4-carboxylic acids and derivatives of carboxylic acids, which has the following advantages: use of environmentally friendly solvents, lower energy consumption, lower consumption of acylating reagents, which allows the corresponding mixtures to be obtained with suitable characteristics and specifications, ease of recovery from the reaction medium and high yields.

Synthesis, Chemical Reactivity, and Antileukemic Activity of 5-Substituted 6,7-Bis(hydroxymethyl)pyrrolothiazole Biscarbamates and the Corresponding Sulfoxides and Sulfones

A series of bis(N-methylcarbamate) and bis derivatives of 5-substituted 6,7-bis(hydroxymethyl)pyrrolothiazoles was prepared.The compounds were tested for activity in vivo against P388 lymphocytic leukemia, and the chemical reactivities of the compounds were compared by using the model nucleophile 4-(4-nitrobenzyl)pyridine (NBP).The 5-(3,4-dichlorophenyl)-substituted biscarbamates 6b, 8b, and 12b were inactive and unreactive toward NBP.The 5-methyl-substituted bicarbamates 6a, 7a, 8a, 9a, 12a, and 13a were all active against murine P388 lymphocytic leukemia.The chemical reactivities of the active compounds depended on the oxidation state of the sulfur.The reactivity toward NBP followed the order S > SO >> SO2.The sulfones 12a and 13a are the most active compounds in this series, and their lack of reactivity toward NBP led to the suggestion that 12a and 13a are activated in vivo.