CAS: 79069-14-0; (S)-Tert-Butyl (1-Hydroxy-3-Methylbutan-2-yl)Carbamate

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L-缬氨酸置于lithium Aluminium Tetrahydride,氯化亚砜,碳酸氢钠体系中,用 四氢呋喃,乙醇 作为反应溶剂,化学反应 7.0H,反应生成 N-Boc-L-缬氨醇
参考文献:通过1,3-偶极环加成反应 迅速进入氨基酸衍生的各种3,4-二氢吡嗪和二氢[1,2,3]三唑并[1,5-A]吡嗪†
标题:通过1,3-偶极环加成反应 迅速进入氨基酸衍生的各种3,4-二氢吡嗪和二氢[1,2,3]三唑并[1,5-A]吡嗪†
摘要:通过分子内1,3-高效,通用和实用地合成各种3,4-二氢吡嗪,6,7-二氢-[1,2,3]三唑并吡嗪和7,8-二氢-[1,2,3]三唑并二氮杂pine描述了从氨基酸衍生的常见中间体以高收率进行偶极环加成.此外,在此方法中,还可以通过一锅获得光学活性的3-芳基取代的6,7-二氢-[1,2,3]三唑并[1,5-A]吡嗪在钯-铜共催化体系中的应用.工作.容易获得的基材和操作简便性使该工艺适合于进一步探索.
DOI:10.1039/c4Ob00639A

专利信息

专利号:US-5869725-A
优先权日:1994-05-17
标 题:Derivatives of aminosulfonic acids, utilization of the same in the synthesis of pseudopeptides and process for their preparation
发明人：GENNARI CESARE; POTENZA DONATELLA; SALOM BARBARA
权利人:PHARMACIA & UPJOHN SPA
摘要:Derivatives of gamma-amino-alpha,beta-unsaturated sulfonic acids, a process for the preparation of the same and their utilization in the synthesis of pseudopeptides characterized by the presence of at least a sulfonamide type bond conjugated to a double bond are described.

专利号:US-6358928-B1
优先权日:1999-11-22
标 题 :Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
发明人：RASNICK DAVID W
权利人:ENZYME SYSTEMS PRODUCTS
摘要:Novel alpha-amino and peptidyl sulfonyl imidazolides, a method for their synthesis, and a method for inhibiting serine proteases therewith are disclosed. Pharmaceutical compositions containing alpha-amino and peptidyl sulfonyl imidazolides and their use in the treatment of disease states characterized by an over-activity of serine proteases are also disclosed. Novel synthetic methods for the synthesis of sulfonyl derivatives, particularly alpha-amino and peptidyl sulfonyl derivatives, from thioic acid S-esters are also disclosed.

专利号:US-7371867-B2
优先权日:2001-02-27
标题 :Non-racemic trifluoroleucine, and methods of making and using
发明人：FICHERA ALFIO; BILGICER ZIHNI; KUMAR KRISHNA; XING XUECHAO
权利人:TUFTS COLLEGE
摘要:One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluoroleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbon-fluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

专利号:EP-0759902-B1
优先权日:1994-05-17
标题:Derivatives of aminosulfonic acids, utilization of the same in the synthesis of pseudopeptides and process for their preparation

专利号:EP-0759902-A1
优先权日:1994-05-17
标题 :Derivatives of aminosulfonic acids, utilization of the same in the synthesis of pseudopeptides and process for their preparation

专利号:US-8129411-B2
优先权日:2005-12-30
标题:Organic compounds
发明人：EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI
权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.