CAS: 3392-05-0; Boc-Ala-Osu

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34404-33-6 3401-36-3 3392-12-9

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Tert-Butyloxycarbonylalanyl-4-Pyridylmethylester置于magnesium,N,N'-二环己基碳二亚胺体系中,用 1,4-二氧六环,甲醇 作为反应溶剂,化学反应 4.0H,反应生成 Boc-L-丙氨酸 N-丁二酰亚胺酯
参考文献:A Mild Method For The Cleavage Of The 4-Picolyloxy Group With Magnesium Under Neutral Conditions
标题:A Mild Method For The Cleavage Of The 4-Picolyloxy Group With Magnesium Under Neutral Conditions
摘要:一种温和且高效的方法被描述,用于在甲醇或水中,以及其他酯类和敏感保护基团存在下,选择性水解4-吡啶甲基酯与镁的作用.此外,4-吡啶甲基芳基醚和硫醚也能顺利地去保护,反应生成相应的酚和硫酚.
DOI:10.1055/s-0031-1290092

专利信息

专利号:US-4148788-A
优先权日:1978-01-23
标 题:Synthesis of thymosin α1
发明人：WANG SU-SUN
权利人:HOFFMANN LA ROCHE
摘要:Thymosin α 1 , was chemically synthesized by the fragment condensation of the protected amino terminal tetradecapeptide with the protected carboxyl terminal tetradecapeptide and by solid phase peptide synthesis. Thymosin α 1 is active as an agent which affects regulation, differentiation and function of thymus dependent lymphocytes (T cells).

专利号:EP-0832096-B1
优先权日:1995-05-04
标题 :Synthesis of proteins by native chemical ligation
发明人：KENT STEPHEN B H; MUIR TOM W; DAWSON PHILIP E
权利人:SCRIPPS RESEARCH INST
摘要:Proteins of moderate size having native peptide backbones are produced by a method of native chemical ligation. Native chemical ligation employs a chemoselective reaction of two unprotected peptide segments to produce a transient thioester-linked intermediate. The transient thioester-linked intermediate then spontaneously undergoes a rearrangement to provide the full length ligation product having a native peptide bond at the ligation site. Full length ligation products are chemically identical to proteins produced by cell free synthesis. Full length ligation products may be refolded and/or oxidized, as allowed, to form native disulfide-containing protein molecules. The technique of native chemical ligation is employable for chemically synthesizing full length proteins.

专利号:US-4891430-A
优先权日:1984-12-04
标 题:Process for synthesizing active esters of carboxylic acids, new alpha-halogenated carbonates which are useful for this synthesis and the method of producing them
发明人：BARCELO GERARD; CASTRO BERTRAND; JAOUADI MAHMOUD; MARTINEZ JEAN; SENET JEAN-PIERRE; SENNYEY GERARD
权利人:INT DES POUDRES ET EXPLOSIFS S
摘要:The invention relates to a new process for preparing active esters or carboyxlic acids, which consists in reacting a carboxylic acid, in the presence of an agent for binding hydrohalic acid, with a carbonate of formula: ##STR1## in which R 1 denotes either a radical of formula ##STR2## in which R 3 and R 4 , which may be identical or different, are not hydrogen atoms and denote organic radicals which may be substituted or unsubstituted and saturated or unsaturated, and may or may not be bound to a polymer, and which can be joined together to form a hetero-cyclic system with the nitrogen, atom, n or a substituted or unsubstituted aryl radical which may or may not be bound to a polymer, n R 2 denotes a hydrogen atom, an aliphatic or cycloaliphatic radical which may be substituted or unsubstituted and saturated or unsaturated, or a substituted or unsubstituted aromatic radical, n and X denotes a halogen atom. n This process is especially useful for the synthesis of active esters of N-protected amino acids. The invention also relates to the new carbonates described above and the method of producing them, which consists in reacting an alpha-halogenated chloroformate of formula: n n R.sup.2 --CHX--O--COCl n n with an alcohol of formula R 1 OH in an inert solvent medium in the presence of an organic or inorganic base.

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-9085605-B2
优先权日:2010-05-27
标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate
发明人：LIU GANG; ZHAO NAN; MA YAO
权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD
摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.

专利号:FR-2574075-A1
优先权日:1984-12-04
标 题 :PROCESS FOR THE SYNTHESIS OF ACTIVE ESTERS OF CARBOXYLIC ACIDS, NOVEL ALPHA-HALOGEN CARBONATES USEFUL FOR THIS SYNTHESIS AND THEIR METHOD OF OBTAINING