CAS: 5241-64-5; Boc-D-Trp-Oh

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112525-72-1 13139-14-5 143824-78-6

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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号54-12-6 色氨酸 | CAS号89037-64-9 Carbonic acid, ... | CAS号171596-28-4 6-表-他达拉非 | CAS号171596-29-5 他达那非 | CAS号249921-19-5 阿拉莫林 | CAS号103429-32-9 D-PHE-CYS-TYR-D... | CAS号103429-31-8 D-PHE-CYS-TYR-D... | CAS号136553-81-6 C: DTRP-DASP-PR... | CAS号158932-00-4 N-B°C-D-色氨醇 | CAS号159634-94-3 N-[N-[(1,1-二甲基乙... | CAS号81377-02-8 司格列肽

二碳酸二叔丁酯,D-色氨酸置于碳酸氢钠,Sodium Carbonate体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 0.25H,以96%的收率获得产物boc-D-色氨酸
参考文献:(+)-诺卡二嗪 B 及其类似物的仿生全合成
标题:(+)-诺卡二嗪 B 及其类似物的仿生全合成
摘要:Nocardioazines A 和 B 是异戊二烯化的,具有生物活性的吡咯并吲哚啉天然产物,从诺卡氏菌中分离出来,具有不对称的环-D-Trp-D-Trp Dkp 核心.基于我们更深入的生物合成理解,(+)-诺卡二嗪 B 的仿生全合成仅需 7 个步骤即可完成,总产率为 23.2%.该途径使用相同数量的步骤并以相似的效率访问 (+)-Nocardioazine B 的区域选择性和立体选择性 C3-异戊二烯化类似物.成功的策略要求尽早执行仿生 C3-异戊二烯化步骤.使用未经保护的色氨酸羧酸导致形成关键中间体exo-12A的高非对映选择性,Exo-12B和exo-12C (>19:1).有证据表明,N 1-甲基化导致异戊二烯化反应分叉,产生 C2-正异戊二烯化异构体.nocardioazine A 具有异戊二烯-环氧化物桥,在多重耐药的哺乳动物结肠癌细胞中抑制 P-糖蛋白 (P-Gp)
DOI:10.1021/acs.Joc.2C01120

专利信息

专利号:US-7122628-B2
优先权日:2000-12-22
标 题:Process for the synthesis of a peptide having a Trp residue
发明人：JACKSON STEVEN ALLEN
权利人:IPSEN MFG IRELAND LTD
摘要:A process for the solid phase synthesis of a peptide having at least one thyptophan residue, wherein said method comprises temporarily protecting the indole ring of said tryptophan residue with a side chain protecting group which is labile to a base wherein said protecting group is removed during cleavage of said peptide from the solid support.

专利号:US-6867202-B1
优先权日:1997-06-25
标 题 :Treatment of insulin resistance
发明人：CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL
权利人:PFIZER
摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

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-4011182-A
优先权日:1975-03-21
标 题:Cyclic undecapeptide analogs of somatostatin and intermediates
发明人：SARANTAKIS DIMITRIOS
权利人:AMERICAN HOME PROD
摘要:Cyclic undecapeptide analogs of somatostatin without cysteine amino acid residues and intermediates obtained in the synthesis of such compounds are described. These cyclic undecapeptides inhibit the secretion of the hormone somatotropin (growth hormone) without materially affecting glucagon levels.

专利号:US-4199500-A
优先权日:1978-11-20
标 题:Peptides related to somatostatin
发明人：SHIELDS JAMES E
权利人:LILLY CO ELI
摘要:The tetradecapaptides of the formula wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit the secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.

专利号:US-4202802-A
优先权日:1978-10-02
标 题 :Peptides related to somatostatin
发明人：SHIELDS JAMES E
权利人:LILLY CO ELI
摘要:The tetradecapeptides of the formula wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly; and X is Ala-Leu, Ala-Phe, Ala-D-Phe, D-Ala-Phe, or D-Ala-Cha; or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.