cPr-PMEDAP
Chemical Name: 2-(2,6-Diamino-N6-cyclopropylpurine-9-yl)ethoxymethylphosphonic acid; N6-Cyclopropyl-2,6-diamino-9-(2-phosphonomethoxyethyl)purine
CAS No. 182798-83-0
项目整合开发状态: Preclinical
项目研究机构: Inst. Organic Chemistry Biochemistry (Originator), Rega Institute for Medical Research (Originator), Gilead (Codevelopment)
合成路线:Alkylation of 2-amino-6-chloropurine (I) with tosylate (II) afforded the phosphonomethoxyethyl purine (III).Subsequent displacement of the chloro atom of (III) by cyclopropylamine (IV) furnished diaminopurine (V).The isopropyl protecting groups of (IV) were finally cleaved by treatment with bromotrimethylsilane.
合成路线:In an alternative method for preparing precursor (V),2-amino-6-chloropurine (I) was first treated with cyclopropylamine (IV) to give diaminopurine (VI),and then alkylated with tosylate (II).
📌 参考资料/链接:
参考文献标题:N6-Substd.nucleotide analogues and their use
文献作者:Holy,A.; De Clercq,E.D.A.(Institute of Organic Chemistry and Biochemistry; Stichting Rega Vzw)
参考来源:US 5977061; WO 9633200