18997-69-8Relevant academic research and scientific papers
The interaction of 4-thiazolidinone derivatives containing indolin-2-one moiety with P-glycoprotein studied using K562 cell lines
Wang, Feng,Liu, Zijian,Wang, Jian,Tao, Jun,Gong, Ping,Bao, Xue,Zhao, Yanfang,Wang, Yulin
, p. 126 - 132 (2015)
P-glycoprotein (P-gp) is an active drug efflux pump, which exists widely in various MDR tumor cells, conferring drug resistance to tumor cells during chemotherapy. Some 4-thiazolidinone derivatives containing indolin-2-one moiety are novel anti-tumor comp
Catalyst-Controlled Transannular Polyketide Cyclization Cascades: Selective Folding of Macrocyclic Polyketides
Raps, Felix C.,F?seke, Vincent C.,H?ussinger, Daniel,Sparr, Christof
supporting information, p. 18390 - 18394 (2020/08/25)
The biomimetic synthesis of aromatic polyketides from macrocyclic substrates by means of catalyst-controlled transannular cyclization cascades is described. The macrocyclic substrates, which feature increased stability and fewer conformational states, were thereby transformed into several distinct polyketide scaffolds. The catalyst-controlled transannular cyclizations selectively led to aromatic polyketides with a defined folding and oxygenation pattern, thus emulating β-keto-processing steps of polyketide biosynthesis.
Synthesis method of 1-(2-dimethylaminoethyl)-5-mercaptotetrazole
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Paragraph 0064; 0065; 0071; 0072, (2020/04/17)
The invention belongs to the technical field of medicines, and particularly relates to a synthesis method of 1-(2-dimethylaminoethyl)-5-mercaptotetrazole. The method comprises the following steps: reacting N, N-dimethylethylenediamine with thiophosgene to obtain isothiocyanate, reacting isothiocyanate with azidotrimethylsilane to obtain 1-(2-dimethylaminoethyl)-5-mercaptotetrazole hydrochloride, dissolving 1-(2-dimethylaminoethyl)-5-mercaptotetrazole hydrochloride in water, and carrying out decolorizing and crystallizing to obtain 1-(2-dimethylaminoethyl)-5-mercaptotetrazole. According to themethod, the isothiocyanate is synthesized from the N, N-dimethylethylenediamine and the thiophosgene through a one-step method, so that the synthesis process is simplified and the yield is greatly increased; non-toxic azidotrimethylsilane is used for replacing virulent sodium azide in the cyclization process, so that the safety of the process is improved, and the method is more suitable for industrial amplification.
Method for simultaneously synthesizing N,N-dimethyl ethylenediamine isothiocyanate and thioacetic acid
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Paragraph 0031-0033; 0036-0038; 0041-0043, (2018/05/16)
The invention relates to a method for simultaneously synthesizing N,N-dimethyl ethylenediamine isothiocyanate and thioacetic acid, and belongs to the field of preparation of medical intermediates. Themethod comprises the following steps: taking N,N-dimethyl ethylenediamine as a starting material; reacting the N,N-dimethyl ethylenediamine with carbon disulfide to prepare thio-inner salt; then reacting the thio-inner salt with acetylchloride to prepare thio-mixed anhydride; and hydrolyzing in an inorganic aqueous alkali at one step to prepare thioacetic acid and N,N-dimethyl ethylenediamine isothiocyanate. By the method, two different valuable products can be obtained simultaneously, operation steps are simplified, and emission of organic by-products is reduced.
Method for preparing isothiocyanate from ethyl chloroformate
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Paragraph 0048, (2018/05/16)
The invention relates to a method for preparing isothiocyanate from ethyl chloroformate. The method comprises the following steps: taking a compound as shown in specification as a starting material, reacting with carbon disulfide to prepare inner salt, and then reacting the inner salt with ethyl chloroformate in an organic solvent at the temperature of 0-40 DEG C to prepare thio-mixed anhydride, wherein in the compound as shown in specification, n is 1, 2, 3, 4 or 5; and adding the mixed anhydride in an inorganic aqueous alkali, and hydrolyzing at the temperature of minus 5-30 DEG C to preparethe corresponding isothiocyanate. According to the preparation method, the mixed anhydride is synthesized at first, and then is hydrolyzed with inorganic alkali, application of organic alkali is avoided effectively, side reaction of the isothiocyanate and alcohol is relieved, and the reaction yield of the isothiocyanate and the purity of the product are improved.
Solid cephalosporin salt
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, (2008/06/13)
A solid cephalosporin derivative having the formula: STR1 wherein X is chlorine or bromine, n is a number from zero to 6, is found to have high stability in storage and may be used as an active component of an antimicrobial composition.
Antibiotic compositions
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, (2008/06/13)
Solid antibiotic compositions containing 7β-[2-(2-imino-4-thiazolin-4-yl)acetamido]-3-{1-[2-(N,N-dimethylamino)ethyl]-1H-tetrazol-5-yl}thiomethyl-3-cephem-4-carboxylic acid dihydrochloride or its hydrate and a pharmaceutically acceptable carbonic acid salt are rapidly converted into an injectable solutions by the addition of a solvent, and the injectable solution shows high antibacterial activity with less local reactions when injected.
