CAS: 402-71-1; (S)-N-(4-Chloro-3-Oxo-1-Phenylbutan-2-yl)-4-Methylbenzenesulfonamide

(S)-N-(4-(Dimethyl(Oxo)-L6-Sulfaneylidene)-3-Oxo-1-Phenylbutan-2-yl)-4-Methylbenzenesulfonamide置于甲烷磺酸,Lithium Chloride体系中,用 四氢呋喃 作为反应溶剂,以2.25 G的收率获得产物n-(对甲苯磺酰基)-L-苯丙氨酰甲基氯酮
参考文献:N-甲苯磺酰基-L-苯丙氨酸氯甲基酮的简便制备
标题:N-甲苯磺酰基-L-苯丙氨酸氯甲基酮的简便制备
摘要:开发了一种简便制备n-甲苯磺酰基-L-苯丙氨酸氯甲基酮的方法.l-苯丙氨酸被甲苯磺酸化并转化为对硝基苯酚的活化酯.随后与二甲基亚砜基亚甲基反应,并用氯化锂和甲磺酸处理,得到α-氯酮.该实用程序避免了使用有毒易爆的重氮甲烷.
DOI:10.2174/157017809790443005

专利信息

专利号:WO-2024153752-A1
优先权日:2023-01-20
标 题 :Stereoselective synthesis of intermediates and synthesis of quinagolids
发明人：RYBERG PER; PINESCHI MAURO; COMPARINI LUCREZIA
权利人:FERRING BV
摘要:Disclosed is a method for preparing compounds with improved stereoselectivities. The described compounds are useful intermediates and may find particular application in the synthesis of compounds containing an octahydrobenzoquinoline moiety (e.g. an octahydrobenzo[g]quinoline moiety), such as quinagolide and its derivatives. Also disclosed is a method for stereoselectively (e.g. enantioselectively) preparing an intermediate used in the existing manufacturing process for the synthesis of quinagolide this intermediate also finding utility in the synthesis of other compounds containing an octahydrobenzo[g]quinoline moiety, in particular those having a substituent at the 3- position on the octahydrobenzo[g]quinoline.

专利号:WO-2024079704-A1
优先权日:2022-10-13
标题 :Synthesis of derivatives of siphonochilone and therapeutic use thereof
发明人：INVERNIZZI LUKE; MOYO PHANANKOSI; MAHARAJ VINESH
权利人:UNIV PRETORIA
摘要:THIS invention relates to the synthesis of derivatives of siphonochilone and therapeutic use thereof in the treatment and prevention of respiratory virus disease, in particular influenza or a coronavirus disease.

专利号:US-7829669-B2
优先权日:1999-06-28
标 题:Catalytically active recombinant memapsin and methods of use thereof
发明人：KOELSCH GERALD; TANG JORDAN J N; HONG LIN; GHOSH ARUN K; LIN XINLI
权利人:OKLAHOMA MED RES FOUND; UNIV ILLINOIS
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogues including isosteres at the sites of the critical amino acid residues were developed and the substrate analogues, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bond to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

专利号:US-4634671-A
优先权日:1982-09-18
标 题 :Water-soluble cross-linked polymer of lysyl endopeptidase, process for preparing same and use of same
发明人：SAKATA YOSHITSUGU; SHINTANI AKINORI; MATSUO TETSUYA; SUGIYAMA HARUHIKO; TOKIOKA NOBUYUKI
权利人:WAKO PURE CHEM IND LTD
摘要:A water-soluble cross-linked polymer of the enzyme lysyl endopeptidase produced by Achromobacter lyticus and a process for preparing the polymer as well as a semi-synthesis of human insulin using the polymer.

专利号:US-2002049303-A1
优先权日:1999-06-28
标 题 :Catalytically active recombinant memapsin and methods of use thereof
发明人：TANG JORDAN J N; LIN XINLI; KOELSCH GERALD; HONG LIN
摘要:Methods for the production of purified, catalytically active, recombinant memapsin 2 have been developed. The substrate and subsite specificity of the catalytically active enzyme have been determined. The substrate and subsite specificity information was used to design substrate analogs of the natural memapsin 2 substrate that can inhibit the function of memapsin 2. The substrate analogs are based on peptide sequences, shown to be related to the natural peptide substrates for memapsin 2. The substrate analogs contain at least one analog of an amide bond which is not capable of being cleaved by memapsin 2. Processes for the synthesis of two substrate analogs including isosteres at the sites of the critical amino acid residues were developed and the substrate analogs, OMR99-1 and OM99-2, were synthesized. OM99-2 is based on an octapeptide Glu-Val-Asn-Leu-Ala-Ala-Glu-Phe (SEQ ID NO:28) with the Leu-Ala peptide bond substituted by a transition-state isostere hydroxyethylene group (FIG. 1 ). The inhibition constant of OM99-2 is 1.6×10 −9 M against recombinant pro-memapsin 2. Crystallography of memapsin 2 bound to this inhibitor was used to determine the three dimensional structure of the protein, as well as the importance of the various residues in binding. This information can be used by those skilled in the art to design new inhibitors, using commercially available software programs and techniques familiar to those in organic chemistry and enzymology, to design new inhibitors to memapsin 2, useful in diagnostics and for the treatment and/or prevention of Alzheimer's disease.

专利号:SA-02230453-B1
优先权日:2001-09-07
标 题 :Methods for the synthesis of conjugate products of an insulin polypeptide with an oligomer, and conjugate products of a proinsulin polypeptide with an oligomer (and methods for their synthesis)