CAS: 5068-28-0; (R)-3-(Benzylthio)-2-((Tert-Butoxycarbonyl)Amino)Propanoic Acid

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📜R-2-苯基-噻唑烷-4-羧酸置于三乙基硅烷,三氟乙酸体系中,用 四氢呋喃,二氯甲烷,水 作为反应溶剂,化学反应生成 Boc-S-苄基-L-半光氨酸
参考文献:引入巯基苄基保护基的两种新方法
标题:引入巯基苄基保护基的两种新方法
摘要:描述了两种新的硫醇苄基化方法:A)用对位取代的苄基阳离子直接进行s-烷基化;b)2-氨基硫醇的还原性s-烷基化.两种方法均提供了以高收率引入苄基型保护基的有效途径.
DOI:10.1016/0040-4039(94)88305-X

专利信息

专利号:US-4786684-A
优先权日:1986-08-21
标题 :Benzylthioether-linked solid support-bound thiol compounds and method for peptide synthesis
发明人：GLASS JOHN D
权利人:SINAI SCHOOL MEDICINE
摘要:A method for the synthesis of sulfydryl-containing peptides which comprises forming a benzylthioether-linked solid support-bound thiol compound having at least one functional group for generating at least one peptide bond, sequentially coupling at least one protected amino acid or peptide to the compound until a peptide having desired amino acid sequence is obtained, and cleaving the benzylthioether linkage to release the peptide from the support with concomitant regenertion of the sulfydryl group in the peptides. The invention also encompasses compounds having the general formula wherein X is H, NH2, or acyl-NHY, said acyl being an amino acid or a peptide; Y is H, COOH, CONHNH2, the ester COOR1 in which R1 is selected from the group consisting of methyl, ethyl, phenyl, ortho-nitrophenyl and para-nitrophenyl, the amide CONH2, or the amide CONHR2 in which R2 is an amino acid or peptide; and providing that X and Y cannot both be H.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-4028315-A
优先权日:1970-10-16
标题:Solid phase synthesis of peptides
发明人：BODANSZKY MIKLOS; SHEEHAN JOHN TIMOTHY
权利人:SQUIBB & SONS INC
摘要:A process for bonding an amino acid to an insoluble hydroxymethyl polymer by esterifying the C-terminal carboxyl group of an N-terminal protected amino acid with the hydroxyl group of an insoluble hydroxymethyl polymer. The esterifying takes place at about room temperature in the presence of a condensing agent. The insoluble hydroxymethyl polymer is a hydroxymethylated copolymer of styrene and divinylbenzene, hydroxymethylcellulose, hydroxymethylated sulfonated polystyrene or polyvinyl alcohol. The condensing agent is dicyclohexylcarbodiimide, carbonyldiimidazole, thionyl chloride, phosphorous oxychloride or ethoxyacetylene. Peptides can be formed by bonding one or more amino acids to the amino acid bonded to the insoluble hydroxymethyl polymer.

专利号:US-4033940-A
优先权日:1975-11-12
标 题:Cyclization of peptides
发明人：HUGHES JOHN L; SEYLER JAY K; LIU ROBERT C
权利人:ARMOUR PHARMA
摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing an amino terminal cystine residue and a cysteine residue located in a position within the amino acid sequence, to give a desired peptide, and placing such intermediate peptide in a solution substantially free of oxygen at a pH of from about 5 to 10 until rearrangement takes place to yield a cyclic disulfide peptide and to displace a molecule of cysteine from the amino terminal cysteine residue. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.

专利号:US-4388235-A
优先权日:1982-02-12
标 题:Synthesis of peptides
发明人：ORLOWSKI RONALD C; SEYLER JAY K
权利人:ARMOUR PHARMA
摘要:New peptides are disclosed which have biological activity of the same type as known calcitonins and which have a shorter amino acid chain than natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.

专利号:US-4217268-A
优先权日:1978-07-20
标 题:Synthesis of peptides
发明人：HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K
权利人:HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K
摘要:A new peptide is disclosed which has biological activity of the same type as known calcitonins and which has a shorter amino acid chain than natural calcitonins. Also resin peptides are disclosed which may be converted to peptides having such biological activity; and processes for producing said resin peptides and said calcitonin peptides.