CAS: 18783-53-4; H-D-Ser(Tbu)-Oh

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128107-47-1 13734-38-8 1676-75-1

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CAS号18822-58-7 O-叔丁基-L-丝氨酸

📜(R)-2-Benzyloxycarbonylamino-3-Tert-Butoxy-Propionic Acid Benzyl Ester置于palladium On Activated Charcoal 氢气体系中,化学反应生成O-叔丁基-D-丝氨酸
参考文献:氨基酸和多肽.第七部分 十四元环二肽dd-,Ll-和dl-Cyclodi-(β-Seryloxypropionyl)的合成
标题:氨基酸和多肽.第七部分 十四元环二肽dd-,Ll-和dl-Cyclodi-(β-Seryloxypropionyl)的合成
摘要:环二-[β-(o-叔丁基-D-丝氨酰氧基)丙酰基]和环二-[β-(o-叔丁基-L-丝氨酰氧基)丙酰基]的合成已通过环二聚反应完成.相关的内消旋(d-大号)的14元环缩酚酸肽的构型中已经制备通过相应的线性缩酚酸肽的环化.这些合成证实,接收性中间体的环二聚主要产生产物的内消旋形式.通过酸对o-叔丁基衍生物的作用,已经制备了具有未保护的丝氨酸残基的类似的环二肽.
Doi:10.1039/j39680001495

专利信息

专利号:WO-2010103857-A1
优先权日:2009-03-12
标 题 :Method for solid-phase synthesis of glycopeptide using silicon-containing protecting group and synthesis device
发明人：NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN
权利人:UNIV HOKKAIDO NAT UNIV CORP; NISHIMURA SHIN-ICHIRO; SHIMAWAKI KEN
摘要:Disclosed are a novel method for the synthesis of a glycopeptide by which glycopeptides of various types can be deprotected and excised from a resin, each under weakly acidic to weakly basic conditions, without causing the problems of the epimerization of an amino acid at the a-position and the ß-elimination of a sugar residue; a synthesis device therefor; and a synthesis intermediate to be used in synthesizing a glycopeptide. Specifically disclosed are a method for the solid-phase synthesis of a glycopeptide which comprises a step for obtaining a glycopeptide derivative wherein the N-terminus is protected, the C-terminus is immobilized to a solid phase via a silicon linker, and a reactive group carried by a sugar residue and a reactive group carried by an amino acid side chain constituting a peptide are protected by silicon-containing groups, and a step for obtaining the glycopeptide by deprotecting said glycopeptide derivative and releasing the same from the solid phase by treating the glycopeptide derivative with an agent for removing the silicon-containing groups and the silicon linker; a synthesis intermediate to be used in the step for obtaining the glycopeptide derivative in the aforesaid method; and a device for the solid-phase synthesis of a glycopeptide.

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.

专利号:US-2009221568-A1
优先权日:2005-11-04
标题:Synthesis of Inhibitors of FtsZ
发明人：SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
权利人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
摘要:FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

专利号:US-11518780-B2
优先权日:2019-07-31
标 题:Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers
发明人：FANG SHIYUE
权利人:FANG SHIYUE
摘要:Embodiments for the synthesis of sensitive oligonucleotides as well as insensitive oligonucleotides are provided. Sulfur-based groups are used for the protection of exo-amino groups of nucleobases, phosphate groups and 2′—OH groups, and as cleavable linker for linking oligonucleotides to a support. Oligonucleotide syntheses are achieved under typical conditions using phosphoramidite chemistry with important modifications. To prevent replacing sulfur-based protecting groups by acyl groups via cap-exchange, special capping agents are used. To retain hydrophobic tag to assist RP HPLC purification, special phosphoramidites are used in the last synthetic cycle. With the sulfur-based groups for protection and linking, oligonucleotide deprotection and cleavage are achieved via oxidation followed by beta-elimination under mild conditions. Therefore, besides for insensitive oligonucleotide synthesis, the embodiments of the invention are capable for the synthesis of oligonucleotide analogs containing sensitive functional groups that cannot survive the harsh conditions used in prior art oligonucleotide synthesis technologies.

专利号:US-9951096-B2
优先权日:2008-08-22
标 题 :Catalysts and methods for polymer synthesis
发明人：ALLEN SCOTT D; CHERIAN ANNA E; SIMONEAU CHRIS A; FARMER JAY J; COATES GEOFFREY W; GRIDNEV ALEXEI; LAPOINTE ROBERT E
权利人:SAUDI ARAMCO TECH CO
摘要:The present invention provides unimolecular metal complexes having increased activity in the copolymerization of carbon dioxide and epoxides. Also provided are methods of using such metal complexes in the synthesis of polymers. According to one aspect, the present invention provides metal complexes comprising an activating species with co-catalytic activity tethered to a multidentate ligand that is coordinated to the active metal center of the complex.

专利号:US-9574189-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries
发明人：FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).