【结 构 式】 |
【分子编号】59321 【品名】 【CA登记号】 |
【 分 子 式 】C20H28B2I3K2N3O13 【 分 子 量 】998.98675 【元素组成】C 24.05% H 2.83% B 2.16% I 38.11% K 7.83% N 4.21% O 20.82% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(IV)In an improved method, the acetamido isophthalamide (I) is treated with boric acid and KOH to form the cyclic diborate tripotassium salt (II). Subsequent alkylation of (II) with 1-chloro-3-methoxy-2-propanol (III) yields regioselectively the N-alkylated acetamide (IV). The borate groups of (IV) are finally removed upon quenching with diluted HCl.
【1】 Bjoersvik, H.-R.; et al.; A selective process for N-alkylation in competition with O-alkylation: Boric acid, borax, and metaborate as a cheap and effective protecting group applicable for industrial-scale synthetic processes. Org Process Res Dev 2001, 5, 5, 472. |
【2】 Priebe, H. (Amersham plc); An N-alkylation. GB 2331098 . |
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