CAS: 581065-95-4; Tert-Butyl 1-Amino-3,6,9,12-Tetraoxapentadecan-15-Oate

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📜在 Palladium On Activated Charcoal,氢气体系中,用 甲醇 作为反应溶剂,50.0 °C,200.0 Kpa 条件下,反应 12.0H,以2080 G的收率获得产物2-[2-[2-[2-(2-叔丁氧羰基乙氧基)乙氧基]乙氧基]乙氧基]乙胺
参考文献:一种氨基聚乙二醇丙酸的制备方法
标题:一种氨基聚乙二醇丙酸的制备方法
摘要:本发明涉及有机合成领域,具体涉及一种氨基聚乙二醇丙酸的制备方法.该制备方法包括:1)将如式i‑2所示的双苄基氨基聚乙二醇丙酸叔丁酯进行催化氢化反应得到如式i‑3所示的氨基聚乙二醇丙酸叔丁酯;2)如式i‑3所示的氨基聚乙二醇丙酸叔丁酯在酸性条件下水解,得到如式i所示的氨基聚乙二醇丙酸.本发明解决了现有技术收率低,危险性高和难以放大生产的缺点.本发明的制备方法,反应条件温和,操作简单,中间体不需提纯即可直接进行下一步反应,总收率高达87‑92%,终产品纯度高达97‑99.5%,为氨基聚乙二醇丙酸的制备提供了一条安全高效的合成路线.

专利信息

专利号:US-2025170267-A1
优先权日:2022-02-28
标 题 :Antibody-drug conjugate precursor and intermediate for synthesis thereof
发明人：TSUZAKI YASUNORI; MIZUNO GEN; KASHIWAGI TAKAMASA; TANAKA MASAYUKI; SHIMIZU HAYATO; NONOUCHI SHIMPEI; MATSUSHITA TAKASHI; KIMURA TOMIO
权利人:UBE CORP
摘要:A method for improving the stability of an antibody-drug conjugate in a living body, and a conjugate precursor for producing a stabilized antibody-drug conjugate. An antibody-drug conjugate precursor represented by the following general formula (I) or a salt thereof, a synthetic intermediate thereof or a salt thereof, n Z-L-D  (I)n n where Z is a reactive group which can react with a functional group present in an antibody or a modified antibody; D is an antitumor drug residue in which one hydrogen atom or one hydroxy group is removed from any position of an antitumor drug molecule or an analog thereof or a derivative thereof; L is a linker which links Z to D; and at least any one of D and L has one or more lactonyl group(s) at any position(s) as substituent(s) or protecting group(s).

专利号:US-11229711-B2
优先权日:2013-06-06
标 题:Linkers for antibody-drug conjugates and related compounds, compositions, and methods of use
发明人：JACKSON DAVID Y; HA EDWARD
权利人:MAGENTA THERAPEUTICS INC
摘要:Provided herein are antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers.