104527-63-1Relevant articles and documents
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Ratner,Clarke
, p. 200,201, 205 (1937)
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Synthetic method for timonacic pharmaceutical intermediate--L-N-acetyl thioproline
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Paragraph 0014; 0015, (2016/10/27)
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%.
Synthesis and biological evaluation of new naphthoquinone-containing pyrrolo-thiazoles as anticancer agents
Lopes, Susana M. M.,Laranjo, Mafalda,Serra, Armenio C.,Abrantes, Ana Margarida,Rocha Gonsalves, Antonio M. D'A.,Botelho, Maria Filomena,Beja, Ana Matos,Silva, Manuela Ramos,Pinho E Melo, Teresa M. V. D.
experimental part, p. 960 - 966 (2010/10/19)
(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.]