📜氯甲酸苄酯 反应生成N-苄氧羰基--6-氨基己酸 参考文献:Method For Making Valproic Acid Derivatives 标题:Method For Making Valproic Acid Derivatives 摘要:本发明揭示了一种制备含有功能化间隔臂的丙戊酸衍生物的方法,所述方法包括将连接到无机基团的间隔臂连接到丙戊酸前体上,制备烷基化化合物,将烷基化合物在液体介质中衍生化制备丙戊酸衍生物,然后从液体介质中分离丙戊酸衍生物.所述丙戊酸衍生物可用于制备免疫反应性丙戊酸共轭物.
专利号:US-4849513-A 优先权日:1983-12-20 标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups 发明人:SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-5118802-A 优先权日:1983-12-20 标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside 发明人:SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-7351852-B2 优先权日:2000-09-05 标题 :T-butoxycarbonylaminoethylamine for the synthesis of PNA monomer units, amino acid derivatives, intermediates therof, and processes for productions of them 发明人:IKEDA HISAFUMI; SAITO ISAO; NAKAMURA YUSHIN 权利人:CREDIA JAPAN CO LTD 摘要:A process for amino acid derivatives shown by the below general formula (I): n n(wherein R 1 means a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms.) having an object to provide a process of the amino acid derivatives of the formula (I) and their synthetic intermediate, t-butoxycarbonylamino-ethylamine, whereby it requires no tedious procedure and is also good in yield, and its application to a mass production is easy, and to provide novel amino acid derivatives of the formula (IV), their synthetic intermediates, and a process thereof, characterized in that it comprises a step to obtain the amino acid derivatives shown by the general formula (I) by hydrolysis of compounds shown by the below formula (II):n n n(wherein R 1 has the same meaning as described above, and R 2 means a straight chain or branched chain alkyl group with 1-4 carbon atoms.) as well as amino acid derivatives shown by the general formula (IV):n n n(wherein R 1 means a hydrogen atom or a straight chain or branched chain alkyl group with 1-5 carbon atoms, and n means any one of integers 1-11.), and a process for the amino acid derivative, characterized in that it comprises a reduction step of benzyloxycarbonyl-ω-amino acid derivatives.
专利号:US-5118800-A 优先权日:1983-12-20 标 题 :Oligonucleotides possessing a primary amino group in the terminal nucleotide 发明人:SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-5015733-A 优先权日:1983-12-20 标题 :Nucleosides possessing blocked aliphatic amino groups 发明人:SMITH LLOYD M; FUND STEVEN; KAISER JR ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieites may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-7417035-B2 优先权日:1998-11-19 标 题:Phospholipid derivatives of non-steroidal anti-inflammatory drugs 发明人:KOZAK ALEXANDER; SHAPIRO ISRAEL 权利人:DPHARM LTD 摘要:Disclosed are compounds having non-steroidal anti-inflammatory drugs (NSAIDS) covalently linked to a phospholipid moiety via a bridging group. Also disclosed are a process for the synthesis of the compounds, pharmaceutical compositions comprising the compounds and the use thereof for the treatment of diseases and disorders related to inflammatory conditions.
[参考文献]: Jianghong An, Et Al. A Novel Small-Molecule Inhibitor Of The Avian Influenza H5N1 Virus Determined Through Computational Screening Against The Neuraminidase. J Med Chem. 2009 May 14;52(9):2667-72.