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Updated: Jul 4, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
简化立体选择性进入 (-) - 基纳戈利德和3 - 替代的八基[g] - 基诺林
Francesca Sardelli1, Lucrezia Margherita Comparini1, Lucilla Favero1
1Department of Pharmacy, University of Pisa, Via Bonanno 33, 56126 Pisa, Italy.
一种新型的立体选择性合成产生了对抗分子纯度的甲基. 这种方法使得能够制备性八化酸诺衍生物,这些衍生物在药物化学中非常有价值.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 合成化学 合成化学
背景情况:
- 螺旋性八化基因基诺林支架是药物化学中的特权结构.
- 对于药物开发而言,对体纯化合物的高效合成至关重要.
研究的目的:
- 为了开发一个简短的立体选择性合成的酶体纯 (3S,4aS,10aR) -quinagolide.
- 建立一种用于制备合性转化3替代性八化[g]诺林的一般方法.
主要方法:
- 用铜催化 (S) -epichlorohydrin与1,6-dimethoxynaphthalene的区域选择性合.
- 一个循环酶胺中间体的灾难选择性转减.
主要成果:
- 实现了非常短的立体选择性合成对抗分子纯 (3S,4aS,10aR) -quinagolide.
- 通过利用化水素双反体和利用减少中的 diastereodivergence,证明了制备各种性转化3替代性八化[g]类的潜力.
结论:
- 开发的合成途径是高效和立体选择性的.
- 这种方法提供了一个通用的平台,可以访问医学上相关的性化诺林.
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