CAS: 152548-66-8; Fmoc-N-Me-Asp(Otbu)-Oh

相似化合物

1799443-40-5 112883-39-3 1676-90-0

上下游产品

CAS号67-56-1 甲醇 | CAS号28920-43-6 芴甲氧羰酰氯(Fm°C-Cl) | CAS号3057-74-7 L-天门冬氨酸-4-叔丁基酯

9-芴甲基-N-琥珀酰亚胺基碳酸酯,N-甲基-L-天冬氨酸β-叔丁基酯置于水,Sodium Hydroxide体系中,用 丙酮 用作溶剂,化学反应 12.0H,以89.5%的收率获得fmoc-N-甲基-L-天冬氨酸 4-叔丁酯
参考文献:一种n-甲基(2S)-2-N-芴甲氧羰基氨基-门冬氨酸(4-叔丁酯)的合成方法
标题:一种n-甲基(2S)-2-N-芴甲氧羰基氨基-门冬氨酸(4-叔丁酯)的合成方法
摘要:本发明涉及一种n‑甲基(2S)‑2‑n‑芴甲氧羰基氨基‑门冬氨酸(4‑叔丁酯)的合成方法.主要解决现在合成方法中产品消旋的技术问题和放大生产问题.本发明经四步合成,第一步,原料a溶解在在四氢呋喃中,加入碳酸铯,然后加入碘甲烷,得到化合物1,产物无需提纯,直接用于下一步反应;第二步,室温下,化合物1在甲醇中通入氢气反应,经钯炭催化得到化合物2;第三步,化合物2溶解在甲醇中,加入l‑(‑)‑二乙酰基酒石酸,经过成盐处理,达到ee>99%,得到化合物3;第四步,化合物3和在丙酮和氢氧化钠中反应,然后加入fmoc‑osu反应,经盐酸酸化,得到目标化合物4.

专利信息

专利号:US-2024067674-A1
优先权日:2020-12-28
标 题 :Method for loading amino acid on resin for solid-phase synthesis
发明人：SEKITA HIROKO; KOMIYA SHIO; DAN KATSUNORI
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:An object of the present invention is to provide a method for efficiently producing a peptide compound of high purity at a high yield. It was found that an amino acid can be efficiently loaded on a resin for solid-phase synthesis by bringing an amino acid solution containing a specific solvent into contact with a resin for solid-phase synthesis that has been swollen with a specific solvent, thereby solving such problem.

专利号:US-12331072-B2
优先权日:2018-11-30
标 题 :Deprotection method and resin removal method in solid-phase reaction for peptide compound or amide compound, and method for producing peptide compound
发明人：IWASAKI KOTARO; KOMIYA SHIO
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:The present inventors found that peptide compounds/amide compounds in which the protecting groups of interest are removed and/or which are removed from resins for solid-phase synthesis can be produced without main chain damage by contacting starting peptide compounds/amide compounds with silylating agents.