136027-17-3Relevant academic research and scientific papers
N-SULFONYLATED PYRAZOLO[3,4-B]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE
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Paragraph 00700; 00724, (2017/04/23)
The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sj?gren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
Preparation method of taurylamine hydrochloride
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Paragraph 0028; 0029; 0030, (2017/01/02)
The invention discloses a preparation method of taurylamine hydrochloride. The preparation method comprises the following steps: by using taurine as an initial raw material, sequentially carrying out amino protecting reaction, chlorination reaction, ammonolysis reaction and deprotection-salification to obtain the taurylamine hydrochloride. The amino protecting group adopted by the amino protecting reaction is benzyl chloroformate, and the amino protecting group is carried out at 5-15 DEG C in the presence of sodium hydroxide and water. The chlorination reagent adopted by the chlorination reaction is thionyl chloride, and the chlorination reaction temperature is 60-70 DEG C. The ammonolysis reaction is carried out in tetrahydrofuran under the action of stronger ammonia water, and the ammonolysis reaction temperature is 5-15 DEG C. The total yield of the four-step reaction can reach 80% or above, the product purity can reach 99% or above, and thus, the method is suitable for industrialized mass production.
Tert -Butyl Hypochlorite Mediated Oxidative Chlorination of S -Alkylisothiourea Salts: Synthesis of Sulfonyl Chlorides
Qiu, Kui,Wang, Rennan
, p. 3186 - 3190 (2015/10/19)
Under neutral conditions, a variety of S-alkylisothiourea salts were smoothly converted into the corresponding sulfonyl chlorides through tert-butyl chlorite mediated oxidative chlorination in good to excellent yields after simple purification. In addition to the environmental and procedural advantages of this method, the neutral conditions potentially make it applicable to substrates that bear acid-sensitive functional groups. For example, the Cbz-protected 2-aminoethanesulfonyl chloride could be synthesized in moderate to good yields under the current neutral conditions, and the acid-sensitive Cbz-protecting group was not affected.
Synthesis of taurine-containing peptides, sulfonopeptides, and N - And O -conjugates
Vertesaljai, Peter,Biswas, Suvendu,Lebedyeva, Iryna,Broggi, Evan,Asiri, Abdullah M.,Katritzky, Alan R.
, p. 2688 - 2693 (2014/04/17)
Taurine-containing water-soluble peptidomimetics were designed and synthesized. N-terminal taurine acylations allowed synthesis of a number of taurine-containing peptides. N-protection of taurine with Cbz and SO 2-activation with benzotriazole followed by coupling with various amino esters, dipeptides and nucleophiles provided taurine N- and O-conjugates and sulfonopeptides.
PROCESS FOR THE PREPARATION OF TAUROLIDINE AND ITS INTERMEDIATES THEREOF
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Paragraph 0026, (2013/09/26)
The present invention relates to a process for the preparation of substantially pure Taurolidine.
4-(SUBSTITUTED ANILINO)QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
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Page/Page column 14, (2012/08/14)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositons and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
4-(Substituted Anilino)-Quinazoline Derivatives Useful as Tyrosine Kinase Inhibitors
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Page/Page column 10, (2012/08/28)
The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
Facile synthesis of hybrid sulfonophosphinodipeptides composing of taurines and 1-aminoalkylphosphinic acids
Meng, Fanhua,He, Fengdan,Song, Xiuqing,Zhang, Leilei,Hu, Wenxiang,Liu, Gang,Xu, Jiaxi
experimental part, p. 423 - 429 (2012/07/28)
Both sulfonopeptides and phosphonopeptides are important analogs of naturally occurring peptides and have been widely used as enzyme inhibitors and haptens for producing catalytic antibodies due to their tetrahedrally structural features. A series of hybr
An efficient and facile synthesis of N-Cbz-β-aminoalkanesulfonamides
Meng, Fanhua,Chen, Ning,Xu, Jiaxi
, p. 2548 - 2553 (2013/06/27)
An efficient method for the synthesis of N-Cbz-β- aminoalkanesulfonamides was described. N-Cbz-β-aminoalkanesulfona-mides were readily prepared in good yields from a variety of amino alcohols, including optically active ones, via N-Cbz protection with ben
'Sulfo-click' for ligation as well as for site-specific conjugation with peptides, fluorophores, and metal chelators
Rijkers, Dirk T. S.,Merkx, Remco,Yim, Cheng-Bin,Brouwer, Arwin J.,Liskamp, Rob M. J.
scheme or table, p. 1 - 5 (2010/11/04)
The 'sulfo-click' reaction, which is a chemoselective amidation reaction involving the reaction of an aminoethane sulfonyl azide with a thio acid, encompasses a new approach for ligation and conjugation. Detailed protocols are provided for decorating biol
