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【结 构 式】

【分子编号】59335

【品名】 

【CA登记号】

【 分 子 式 】C16H19B2I3K3N3O12

【 分 子 量 】964.97019

【元素组成】C 19.92% H 1.98% B 2.24% I 39.45% K 12.16% N 4.35% O 19.9%

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:(II)

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 2-chloroethanol (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 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 59234 (3R)-3-hydroxy-3-phenylpropyl 4-methylbenzenesulfonate C16H18O4S 详情 详情
(II) 59335   C16H19B2I3K3N3O12 详情 详情
(III) 10384 2-Chloro-1-ethanol; Ethylene chlorohydrin 107-07-3 C2H5ClO 详情 详情
(IV) 59336   C18H24B2I3K2N3O13 详情 详情
Extended Information