CAS: 1499-55-4; H-Glu(Ome)-Oh

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(S)-Methyl-3-(5'-Oxo-9λ4-Boraspiro[bicyclo[3.3.1]Nonane-9,2'-[1,3,2]Oxazaborolidin]-4'-yl)Propanoate置于四丁基氟化铵体系中,用 四氢呋喃,水 用作溶剂,化学反应 5.0H,以81%的收率获得l-谷氨酸-5-甲酯
参考文献:四丁基氟化铵作为一种温和且通用的试剂,用于将硼恶唑烷酮裂解为相应的游离 α-氨基酸
标题:四丁基氟化铵作为一种温和且通用的试剂,用于将硼恶唑烷酮裂解为相应的游离 α-氨基酸
摘要:用 9-硼双环 [3.3.1] 壬烷 (9-Bbn) 保护 α-氨基酸以得到相应的硼恶唑烷酮非常有吸引力,因为它同时掩盖了氨基和羧酸官能团.然而,脱保护所需的苛刻方法限制了其使用.在这里,我们报告四丁基氟化铵 (Tbaf) 是一种温和且通用的试剂,可将硼恶唑烷酮裂解为相应的游离 α-氨基酸.研究了反应条件,包括使用各种亲核氟化物源,溶剂和反应温度.包含铵阳离子的亲核氟化物源证明优于其他抗衡阳离子.反应范围扩展到 B,B-二苯基-和 B,B-二乙基硼恶唑烷酮配合物的裂解.此外,
Doi:10.1002/ejoc.201700063

专利信息

专利号:WO-9600391-A1
优先权日:1994-06-23
标题:Methods for the synthesis of diketopiperazines
发明人：CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
权利人:AFFYMAX TECH NV; CAMPBELL DAVID; GALLOP MARK A; GORDON ERIC M; LOOK GARY C; PATEL DINESH; SZARDENINGS ANNA KATRIN
摘要:Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.

专利号:US-10377699-B2
优先权日:2013-11-06
标 题 :Daptomycin analogues and a method for the preparation of daptomycin or a daptomycin analogue
发明人：LI XUECHEN; LAM HIU YUNG
权利人:UNIV HONG KONG
摘要:A method for the synthesis of daptomycin or a daptomycin analog is carried out on a resin to form a linear precursor followed by a serine ligation macrocyclization in solution. Daptomycin analogs can differ from daptomycin by substitution of amino acids residues and/or deletion or addition of amino acid residues. Daptomycin analogs can include a different fatty acid in the side arm of the daptomycin analog.

专利号:US-5780579-A
优先权日:1993-08-10
标题:Method for the preparation of polyamino acids
发明人：SOULA GERARD; GROSSELIN JEAN-MICHEL; JORDA RAFAEEL; CASTAN CATHERINE
权利人:FLAMEL TECH SA
摘要:PCT No. PCT/FR94/00992 Sec. 371 Date Mar. 28, 1996 Sec. 102(e) Date Mar. 28, 1996 PCT Filed Aug. 9, 1994 PCT Pub. No. WO95/04772 PCT Pub. Date Feb. 16, 1995The present invention relates to a method for the preparation of polyamino acids, with controlled molecular weights, by polymerization of N-carboxyanhydrides (NCAs) of at least one amino acid, using at least one initiator of the strong base type and in liquid medium, characterized in that it consists in including, in the liquid reaction medium, given amounts of water and/or of alcohol. Application: synthesis of polyamino acids with mechanical and rheological characteristics adapted to applications as biomaterials.

专利号:US-8487108-B2
优先权日:2005-11-14
标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
发明人：BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

专利号:US-4588825-A
优先权日:1983-10-11
标 题 :Intermediates for the synthesis of 4-amino-4,5-dihydro-2-furancarboxylic acid
发明人：BURKHART JOSEPH P; HOLBERT GENE W
权利人:MERRELL DOW PHARMA
摘要:This application relates to a stereospecific process for preparing specific enantiomers of 4-amino-4,5-dihydro-2-furancarboxylic acid and C 1-6 lower alkyl esters thereof. These compounds are γ-aminobutyric acid transaminase inhibitors useful in the treatment of epilepsy.

专利号:US-10407468-B2
优先权日:2016-03-23
标 题 :Methods for synthesizing α4β7 peptide antagonists
发明人：BHANDARI ASHOK; MANTHATI SURESH KUMAR; MEHROTRA MUKUND M; ANANDAN SAMPATH-KUMAR; PATEL DINESH V
权利人:PROTAGONIST THERAPEUTICS INC
摘要:The present invention provides methods of making α4β7 peptide monomer and dimer antagonists. Methods of the present invention include solid phase and solution phase methods, as well as synthesis via condensation of smaller peptide fragments. Methods of the present invention further include methods directed to the synthesis of peptides comprising one or more penicillamine residues.