52530-50-4Relevant articles and documents
SuFExable Isocyanides for Ugi Reaction: Synthesis of Sulfonyl Fluoro Peptides
Xu, Shuheng,Cui, Sunliang
, p. 5197 - 5202 (2021/07/20)
Herein, the sulfonyl fluoro isocyanides were first developed as a new type of SuFExable synthon, and they are used as building blocks in the Ugi reaction (U-4CR). The Ugi reaction was established and the substrate scope was investigated, and various sulfonyl fluoro α-amino amides and peptides could be reached in a one-step synthesis. Therefore, this protocol opens a new vision for SuFExable building blocks and click chemistry, and it also provides a distinct approach to sulfonyl fluoro peptides.
Preparation method of taurylamine hydrochloride
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, (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.
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.
