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新型强效抗支气管痉挛剂7-[(2,2-二甲基)丙基]-1-甲基黄嘌呤的合成与分析概况

Synthesis and analytical profile of the new potent antibronchospastic agent 7-[(2,2-dimethyl)propyl]-1-methyl xanthine.

作者信息

Agostini O, Bonacchi G, Coppini G, Di Marco G, Paoli P, Toja E

机构信息

Istituto Farmacobiologico Malesci S.p.A., Research Laboratories, Florence, Italy.

出版信息

Arzneimittelforschung. 1995 Jun;45(6):684-8.

PMID:7646571
Abstract

7-[(2,2-Dimethyl)propyl]-1-methyl xanthine (CAS 155006-67-0, MX2/120) is a new potent antibronchospastic agent with negligible side effects. The synthesis involves the alkylation of 3-benzyl-1-methyl xanthine with neopentyl bromide followed by removal of the benzyl protecting group. Main physico-chemical properties were determined using NMR, MS, IR, UV spectra and X-ray crystal structure. A quantitative determination of substances related to MX2/120 and of residual solvents by means of HPLC and GC, respectively, is described. MX2/120 is safely stored at room temperature for a long time.

摘要

7-[(2,2-二甲基)丙基]-1-甲基黄嘌呤(CAS 155006-67-0,MX2/120)是一种新型强效抗支气管痉挛剂,副作用可忽略不计。其合成过程包括用新戊基溴对3-苄基-1-甲基黄嘌呤进行烷基化,然后去除苄基保护基团。利用核磁共振(NMR)、质谱(MS)、红外光谱(IR)、紫外光谱(UV)和X射线晶体结构测定了主要物理化学性质。分别描述了通过高效液相色谱(HPLC)和气相色谱(GC)对与MX2/120相关的物质和残留溶剂进行定量测定的方法。MX2/120在室温下可长期安全储存。

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