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Tert-Butyl (4S,4'S,5'R)-4-Amino-5-(3',4'-Dimethyl-2'-Oxo-5'-Phenyl-1'-Imidazolydinyl)-5-Oxopentanoate置于水体系中,化学反应 12.0H,以45%的收率获得产物l-焦谷氨酸
参考文献:1,5-二甲基-4-苯基咪唑啉二-2-酮衍生的亚氨基糖苷:有用的新试剂,用于实际不对称合成α-氨基酸.
标题:1,5-二甲基-4-苯基咪唑啉二-2-酮衍生的亚氨基糖苷:有用的新试剂,用于实际不对称合成α-氨基酸.
摘要:已制备了新的1,5-二甲基-4-苯基咪唑啉二-2-酮衍生的无环手性亚胺基甘氨酸试剂,并在(a)强碱(lhmds,Kobu)下,在氯化锂存在下,用活化的烷基卤化物和亲电烯烃非对映选择性烷基化. (t))和低温(-78摄氏度)条件,(b)固液相转移催化反应(lioh,Tbab,-20摄氏度)条件和(c)在有机碱(dbu)存在下,Bemp,Tmg,-20摄氏度).在双亲电子试剂的情况下,发生c-和n-烷基化以提供杂环衍生物.(a)用liooh或lioh分两步进行水解,然后进行酸性水解或dowex纯化,(b)在回流水中一步一步得到相应的α-氨基酸,进行了烷基化产物的水解.(c)在甲醇中的dbu存在下提供n-保护的α-氨基酸甲酯,或(d)通过保护-水解程序得到n-Boc保护的α-氨基酸.通常已以非常好的收率回收了手性咪唑啉酮.已经证明该方法对于合成无环和杂环的(S)-和(R)-α-氨基酸是有用的.
DOI:10.1021/jo000321T

专利信息

专利号:US-11926589-B2
优先权日:2019-07-09
标 题 :Process for the synthesis of non-racemic cyclohexenes
发明人：REISMAN SARAH; ROMBOLA MICHAEL; LADD CAROLYN L; MCLAUGHLIN MARTIN JOHN; ZUEND STEPHAN; GOETZ ROLAND
权利人:BASF CORP; CALIFORNIA INST OF TECHN
摘要:This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R 10a , R 10b , R 10c , R 10d , R 10a′ , R 10b′ , R 10c′ , R 10d′ , Z and Z′ have the meanings as defined in the description.

专利号:WO-2023030277-A1
优先权日:2021-08-30
标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog
发明人：SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN
权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD
摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.

专利号:US-2022395800-A1
优先权日:2019-11-04
标题:Device for automated synthesis of oligo- and polysaccharides
发明人：SEEBERGER PETER H; DANGLAD FLORES JOSE; LE MAI HOANG KIM; PARDO VARGAS ALONSO; SLETTEN ERIC; SALWICZEK MARIO
权利人:MAX PLANCK GESELLSCHAT ZU RFERDERUNG DER WSS E V; GlycoUniverse GmbH & Co KG&A
摘要:The present invention generally relates to automated synthesis technology, and more particularly, to a device and method for automated synthesis of oligo- and polysaccharides on a solid support. In particular the present invention relates to a device for automated synthesis of oligo- and polysaccharides on a solid support comprising a reaction vessel, a reagent storing component, a reagent delivery system, a cooling device for cooling reaction vessel, and a pre-cooling device for pre-cooling the reagents to be supplied.

专利号:US-2023313255-A1
优先权日:2020-07-15
标题:Massively Parallel Enzymatic Synthesis of Polynucleotides
发明人：HORGAN ADRIAN; LACHAIZE HENRI; VERARDO DOMIANO; GODRON XAVIER
权利人:DNA SCRIPT
摘要:The invention is directed to methods and compositions for inkjet assisted synthesis of a plurality of polynucleotides at reaction sites on a substrate using template-free polymerases, such as, terminal deoxynucleotidyl transferases (TdTs). Compositions of the invention include formulations of synthesis reagents for inkjet delivery including, but not limited to, TdT coupling reaction buffers and 3′-O-protected dNTP monomers.

专利号:US-2004249170-A1
优先权日:2002-01-24
标 题 :Process for preparing an intermediate useful for the asymmetric synthesis of duloxetine
发明人：BORGHESE ALFIO
摘要:This invention provides a process for the synthesis of(S)-3-Methylamino-1-2-thienyl)-1-propanol, a key intermediate in the synthesis of duloxetine.

专利号:US-2006287520-A1
优先权日:2005-05-16
标 题 :Synthesis of salinosporamide A and analogues thereof
发明人：DANISHEFSKY SAMUEL J; ENDO ATSUSHI
权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.