CAS: 7536-58-5; Boc-Asp(Obzl)-Oh

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2177-63-1 3479-47-8 51186-58-4

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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号2177-63-1 L-天冬氨酸-β-苄酯 | CAS号1361400-95-4 α-picolyl N-B°C... | CAS号2886-33-1 L-天冬氨酸双苄酯对甲苯磺酸盐 | CAS号104-15-4 对甲苯磺酸 | CAS号30750-74-4 B°C-L-天冬氨酸酐 | CAS号100-51-6 苯甲醇 | CAS号56-84-8 L-天门冬氨酸 | CAS号34582-32-6 N-叔丁氧羰基-L-天冬氨酸 1-叔丁酯 | CAS号23446-11-9 B°C-MET-GLY-TRP... | CAS号83345-44-2 (S)-3-((叔丁氧基羰基)... | CAS号81323-58-2 N-(叔丁氧基羰基)-(s)-... | CAS号26048-69-1 N-[叔丁氧羰基]-L-天冬氨... | CAS号65710-57-8 N-叔丁氧羰基-3-[(苄氧羰... | CAS号59768-74-0 B°C-L-天冬氨酸4-甲酯 | CAS号6327-59-9 L-天门冬氨酸二苄酯盐酸盐 | CAS号104227-71-6 (S)-B°C-3-氨基-Y-丁内酯

L-天冬氨酸双苄酯对甲苯磺酸盐置于三乙胺体系中,用 四氢呋喃,乙醇,水 作为反应溶剂,化学反应 14.0H,反应生成 Boc-L-天冬氨酸 4-苄酯
参考文献:Chirospecific Synthesis Of (1S,3R)-1-Amino-3-(Hydroxymethyl)Cyclopentane,Precursor For Carbocyclic Nucleoside Synthesis. Dieckmann Cyclization With An .Alpha.-Amino Acid
标题:Chirospecific Synthesis Of (1S,3R)-1-Amino-3-(Hydroxymethyl)Cyclopentane,Precursor For Carbocyclic Nucleoside Synthesis. Dieckmann Cyclization With An .Alpha.-Amino Acid
摘要:Carbocyclic Nucleosides Are Important Isosteres Of Nucleosides Possessing A Variety Of Antiviral And Antineoplastic Activities. We Report Here A New Method For The Chirospecific Synthesis Of (1S,3R)-1-Amino-3-(Hydroxymethyl)Cyclopentane. This Compound Is A Key Precursor For The Synthesis Of Some Carbocyclic Nucleosides. The Method Involves (1) An Improved Synthesis Of (S)-2-Aminoadipic Acid; (2) Dieckmann Cyclization Of This Alpha-Amino Acid To An Aminocyclopentanone; And (3) Elaboration Of The Latter To The Target (1S,3R)-L-Amino-3-(Hydroxymethyl)Cyclopentane. The Starting (S)-2-Aminoadipic Acid Delta-Methyl Ester Was Prepared Enantiomerically Pure From (S)-Aspartic Acid In 51% Overall Yield. Dieckmann Condensation Converted This Amino Acid To A (Methoxycarbonyl)-Cyclopentanone,And Reduction Of The Ketone Followed By Elimination Yielded (S)-3-[n-(9-Phenylfluoren-9-yl)Amino]-1-(Methoxycarbonyl)Cyclopentene. Reduction Of The Double Bond Gave A Mixture Of The Cis And Trans Diastereomers. This Mixture Was Converted To A Single Diastereomer By Epimerization And Trapping Of The Cis Isomer As (1S,4R)-2-(9-Phenylfluoren-9-yl)-2-Azabicyclo[2.2.1]Heptan-3-One. Hydrolytic Cleavage Of The Lactam Followed By Reduction Gave (Is,3R)-1-Amino-3-(Hydroxymethyl)-Cyclopentane.
DOI:10.1021/jo00061A006

专利信息

专利号:WO-9312076-A1
优先权日:1991-12-13
标题:Reagents for automated synthesis of peptide analogs
发明人：WEBB THOMAS ROY
权利人:CORVAS INT INC
摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.

专利号:US-2007179279-A1
优先权日:2005-12-30
标题:Methods for the synthesis of arginine-containing peptides
发明人：CHEN LIN; ROBERTS CHRISTOPHER R
权利人:CHEN LIN; ROBERTS CHRISTOPHER R
摘要:Methods for the synthesis of arginine-containing peptides are provided. The methods include a step that minimizes contact of side chain protected arginine with base prior to the coupling step.

专利号:US-4704450-A
优先权日:1983-02-21
标 题 :Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate peptides
发明人：DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY
权利人:SANOFI SA
摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

专利号:US-4581168-A
优先权日:1983-02-21
标题:Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides
发明人：DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY
权利人:SANOFI SA
摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

专利号:US-5886104-A
优先权日:1993-06-18
标题 :Grafted cross-linked polyolefin substrates for peptide synthesis and assays
发明人：PEDERSEN WALTHER BATSBERG; ALMDAL KRISTOFFER; WINTHER LARS; BERG ROLF HENRIK
权利人:FORSKNIINGSCENTER RISO
摘要:A solid support for the solid-phase synthesis of peptides or proteins in high yield and in high purity, suited both to the synthesis of a single peptide or protein and to the parallel and substantially simultaneous synthesis of a plurality thereof, is based on a cross-linked polyolefin, especially polyethylene, substrate, the cross-linking having been obtained by irradiation with high energy electrons or γ radiation or treatment with organic peroxide such as benzoyl peroxide, to which substrate are grafted polymer chains such as polystyrene chains which are functionalized with a chemical functionality facilitating the formation of an anchoring linkage between the polymer moiety and another chemical species. The solid support is also suited for use in solid-phase biosystems, notably bioassays, such as immunoassays, DNA hybridization assays or PCR amplification. The grafted chains may bear substituents which are such that the polymer-grafted cross-linked polyolefin substrate is swellable by water or aqueous media, in other words, hydrophilic, which makes the solid support particularly well suited for assays of the ELISA type.

专利号:EP-0433345-B1
优先权日:1988-09-01
标题:Peptide synthesis method and solid support for use in the method
发明人：BERG ROLF H; ALMDAL KRISTOFFER; PEDERSEN WALTHER BATSBERG; HOLM ARNE; TAM JAMES P; MERRIFIELD ROBERT BRUCE
权利人:RISOE FORSKNINGSCENTER
摘要:A method for the solid-phase synthesis of peptides or proteins in high yield and high purity uses a solid support consisting of a functionalized polystyrene-grafted polymer substrate, the grafted polystyrene chains being substantially non-cross-linked and having a chain molecular weight, not including optional non-reactive substituents, of at least 200,000, preferably in the range of 600,000-1,200,000. Particularly suitable polymer substrates are substrates of a polyolefin such as polyethylene. The method is particularly well-suited to the compartmentalized synthesis of a multitude of peptides or proteins in a parallel and substantially simultaneous fashion. Preferred embodiments of a solid support for performing the synthesis are prepared from thin polyethylene sheet or film which has been grafted with polystyrene chains in a radical-initiated process in which the polyethylene sheet or film is immersed in a solution of optionally substituted styrene monomer in an alcohol such as methanol, the volume percentage of styrene in the solution preferably being about 30 % v/v, and subjected to gamma irradiation.