CAS: 88899-55-2; Oxacyclohexadeca-3,5,11,13-Tetraen-2-One, 8-Hydroxy-16-[(1S,2R,3S)-2-Hydroxy-1-Methyl-3-[(2R,4R,5S,6R)-Tetrahydro-2,4-Dihydroxy-5-Methyl-6-(1-Methylethyl)-2H-Pyran-2-Yl]Butyl]-3,15-Dimethoxy-5,7,9,11-Tetramethyl-, (3Z,5E,7R,8S,9S,11E,13E,15S,16R)-

上下游产品

CAS号243468-81-7 | CAS号381246-92-0 (2S,4S,5S)-7-me... | CAS号381247-15-0 (4R,5S,6S,E)-et... | CAS号381246-91-9 (3R,4S,5S)-4-be...

📜(3Z,5E,7R,8S,9S,11E,13E,15S,16R)-16-[(2R,3R,4S,7R,8S,9R)-3,9-Bis[[tert-Butyl(Dimethyl)Silyl]Oxy]-7-Hydroxy-4,8,10-Trimethyl-5-Oxoundecan-2-Yl]-3,15-Dimethoxy-5,7,9,11-Tetramethyl-8-Triethylsilyloxy-1-Oxacyclohexadeca-3,5,11,13-Tetraen-2-One置于三(二甲氨基)锍二氟三甲基硅酸,水体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 4.0H,以93%的收率获得产物巴佛洛霉素a1
参考文献:(-)-Bafilomycin A1的全合成:非对映选择性巴豆基硼化和甲基酮醛醇缩合反应的应用.
标题:(-)-Bafilomycin A1的全合成:非对映选择性巴豆基硼化和甲基酮醛醇缩合反应的应用.
摘要:精心策划保护基团是大环内酯类抗生素bafilomycin A 1(1)的全合成的基本要求.关键步骤是在封闭大环之前,两个先进的,适当保护的中间体的suzuki交叉偶联反应,以及高度立体选择性的甲基酮醇醛缩合反应.
DOI:10.1002/(Sici)1521-3773(19990601)38:11<1652::Aid-Anie1652>3.0.Co;2-K

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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-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:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:US-2025041330-A1
优先权日:2022-02-11
标题:Method of treating obesity by selective targeting of visceral adiposity using polycation nanomedicine
发明人：QIANG LI; LEONG KAM W; Huang Baoding; WAN QIANFEN
权利人:UNIV COLUMBIA
摘要:The method of treating obesity and targeting adipose tissue in a patient may use injection of a polycationic polymer, such as polyamidoamine (PAMAM) generation 3 (P-G3) or a PCL-g-PAMAM Denpol, that when delivered intraperitoneally, selectively targets visceral adiposity due to its high charge density. P-G3 treatment of obese mice inhibits visceral adiposity, increases energy expenditure, prevents obesity, and alleviates associated metabolic dysfunctions. The extracellular matrix of adipose tissue is enriched with glycosaminoglycans, the known biomacromolecules with the strongest negative charge. P-G3 uncouples adipocyte lipid synthesis and storage from adipocyte development, creating adipocytes with normal functions but that are deficient in hypertrophic growth. The visceral fat distribution of P-G3 is further enhanced by modifying P-G3 with cholesterol to form lipophilic nanoparticles, effective in treating obesity. This strategy provides a method to target visceral adiposity, and cationic nanomaterials useful for treating metabolic diseases or for delivery of additional treating agents.