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📜氯甲酸苄酯置于三乙胺体系中,用 水,乙腈 作为反应溶剂,化学反应 5.0H,反应生成 N-苄氧羰基-L-丙氨酸 N-羟基琥珀酰亚胺酯
参考文献:水溶液中的肽合成.一,对二烷基磺基苯酚作为水溶性偶联剂的应用
标题:水溶液中的肽合成.一,对二烷基磺基苯酚作为水溶性偶联剂的应用
摘要:发现(对羟基苯基)二甲基锍甲基硫酸盐(Hodmsp.meso4-)是一种非常好的偶联剂,具有水溶性和高反应性;在反应性,产品纯度和外消旋化方面,它与通常的活性酯一样令人满意.hodmsp.meso4-活性酯法的显着优势在于,当反应混合物的ph值得到控制时,双功能残基如arg,Lys,Cys和tyr可以被选择性地酰化.通过这种新的活性酯方法合成了软体动物神经肽 Fmrfamide(phe-Met-Arg-Phe-Nh2),以评估该方法在涉及肽合成的进一步应用中的应用.
DOI:10.1246/bcsj.60.2409

专利信息

专利号:US-4504415-A
优先权日:1983-04-04
标题:Synthesis of thymosin α1 and desacetyl thymosin α1
发明人：FELIX ARTHUR M; GILLESSEN DIETER; STUDER ROLF; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD
权利人:HOFFMANN LA ROCHE
摘要:An improved solution phase synthesis of thymosin alpha 1 and desacetyl thymosin alpha 1 with t-Boc side chain protection and proceeding through novel intermediates is disclosed.

专利号:WO-0071569-A1
优先权日:1999-05-26
标题 :Minimal isolation peptide synthesis process using ion-exchange resins as scavenging agents
发明人：TOLLE JOHN C; CALIFANO JEAN-CHRISTOPHE; DHAON MADHUP K; SACHS HOWARD A; BLODGETT JAMES K
权利人:ABBOTT LAB
摘要:A process for the production of a polypeptide having a pre-determined number and sequence of amino acid residues, comprising the steps of first exposing a first substrate amino acid or peptide fragment to a stoichiometric excess of a second reactant amino acid or peptide fragment to form a condensation product; second, contacting the reaction solution from the first step with an insoluble scavenger to sequester the excess of the second reactant amino acid or peptide fragment; third, removing from the solution the sequestered excess second reactant amino acid or peptide fragment; fourth, subjecting the reaction solution to a reaction which removes the protecting group from either the N- or C-terminus of the condensation product of the first step; and fifth, if necessary, repeating the first through fourth steps. The method is capable of large-scale production of peptides in solution, is not subject to the one-terminus-only limitation of the solid-phase method, possesses the 'cleanliness' of the solid-phase method and, like the solid-phase method, is capable of automation. Most importantly, however, the method of the present invention does not require the frequent isolation of intermediates in a lengthy synthetic sequence nor, necessarily, the removal of all contaminating by-products from the reaction mixture prior to subsequent processing steps.

专利号:MX-PA01012082-A
优先权日:1999-05-26
标 题 :SYNTHESIS PROCESS OF MINIMUM INSULATION PEPTIDES, USING ION EXCHANGE RESINS AS CLEANING AGENTS.