119225-23-9Relevant academic research and scientific papers
Preparation method of taurylamine hydrochloride
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Paragraph 0022; 0023; 0024, (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.
PROCESS FOR THE PREPARATION OF TAUROLIDINE AND ITS INTERMEDIATES THEREOF
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Page/Page column 4, (2012/06/15)
The present invention relates to a process for the preparation of substantially pure Taurolidine.
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
scheme or table, 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
Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap
Brouwer, Arwin J.,Ceylan, Tarik,Jonker, Anika M.,Linden, Tima Van Der,Liskamp, Rob M.J.
scheme or table, p. 2397 - 2406 (2011/05/12)
We have designed and synthesized novel irreversible serine protease inhibitors containing aliphatic sulfonyl fluorides as an electrophilic trap. These substituted taurine sulfonyl fluorides derived from taurine or protected amino acids were conveniently s
First and convergent synthesis of hybrid sulfonophosphinopeptides
He, Fengdan,Meng, Fanhua,Song, Xiuqing,Hu, Wenxiang,Xu, Jiaxi
scheme or table, p. 3922 - 3925 (2009/12/05)
Figure Presented Hybrid sulfonophosphinopeptides were first and convergently synthesized in satisfactory to good yields via the Mannich-type reaction of N-protected 2-aminoalkanesulfonamides, aromatic aldehydes, and aryldichlorophosphines and subsequent aminolysis with amino esters.
Synthesis and applications of β-aminoethanesulfonyl azides
Brouwer, Arwin J.,Merkx, Remco,Dabrowska, Katarzyna,Rijkers, Dirk T. S.,Liskamp, Rob M. J.
, p. 455 - 460 (2007/10/03)
A very efficient method for the synthesis of β-aminoethanesulfonyl azides is descibed. These aliphatic sulfonyl azides are accessible starting from a variety of protected amino acids, including those having functionalized side chains. Furthermore, these s
N - ( 2 - aryl - propionyl ) - sulfonamides and pharmaceutical preparations containing them
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, (2008/06/13)
The compounds of formula 1, wherein R and R2 are as defined in the disclosure, are useful in the prevention and treatment of tissue damage due to exacerbated recruitment of polymorphonuclear neutrophils (PMN leukocytes) at the inflammatory sites.
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
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, (2008/06/13)
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the
Amino acid derivatives with anticonvulsant activity
Paruszewski,Strupinska,Stables,Swiader,Czuczwar,Kleinrok,Turski
, p. 629 - 631 (2007/10/03)
A series of benzylamides of N-alkylated, N-acylated or free nine cyclic and one linear amino acids as potential anticonvulsants have been synthesized. The structures of the obtained compounds were designed on the basis of the previously determined structure and physicochemical properties/anticvonvulsant activity relationship of the formerly synthesized compounds of this type. The obtained compounds were evaluated in mice after intraperitoneal (ip) administration, by maximal electroshock seizure test (MES test), subcutaneous (sc) pentylenetetrazol test (sc PTZ test) and by the rotarod neurotoxicity test (Tox test). The results were the basis for their classification into one of three classes of the Anticonvulsant Screening Project (ASP) of the Antiepileptic Drug Development Program (ADDP) of the NIH. Three selected compounds were tested quantitatively in rats after oral administration. The MES ED50, sc PTZ ED50, Tox TD50 were determined and their protective index (PI) values were calculated. Anticonvulsant activity of the most promising compound (15) was examined in different seizure models. The respective ED50 and PI values of this compound were as follows: against bicuculline, 73 and 1.4; against PTZ, 47 and 2.2; against strychnine, 73 and 1.4; against pilocarpine 156, and 0.7; against kainic acid (2-carboxy-4-isopropenyl-3-pyrrolidineacetic acid), 39 and 2.6; against AMPA (α-amino-3-hydroxy-5methyl-4-isoxazolepropionic acid), 10 and 10.3 and against NMDA (N-methyl-D-Aspartic acid), 114 and 0.9.
Synthesis of RGD analogs as potential vectors for targeted drug delivery
Jiang, Ji,Wang, Wei,Sane, David C.,Wang, Binghe
, p. 357 - 379 (2007/10/03)
RGD analogs bind to integrin receptors with high affinity and therefore have the potential to be used as vectors for the targeted delivery of pharmaceutical agents to designated sites. Critical to this application is the ability to synthesize RGD analogs
