Rapid Catalyst Identification for the Synthesis of the Pyrimidinone Core of HIV Integrase Inhibitors

被引：51

作者：

Bellomo, Ana ^{[2
]}

Celebi-Olcum, Nihan ^{[1
]}

Bu, Xiaodong ^{[3
]}

Rivera, Nelo ^{[3
]}

Ruck, Rebecca T. ^{[3
]}

Welch, Christopher J. ^{[3
]}

Houk, Kendall N. ^{[1
]}

Dreher, Spencer D. ^{[3
]}

机构：

[1] Univ Calif Los Angeles, Dept Chem & Biochem, Los Angeles, CA 90095 USA

[2] Univ Penn, Dept Chem, Philadelphia, PA 19104 USA

[3] Merck Res Labs, Dept Proc Chem, Rahway, NJ 07065 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2012年 / 51卷 / 28期

基金：

美国国家科学基金会;

关键词：

heterocycles; high-throughput screening; homogeneous catalysis; P ligands; synthetic methods; ARYL CHLORIDES; DISCOVERY; DERIVATIVES; ACID; RALTEGRAVIR; ESTER;

D O I：

10.1002/anie.201201720

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A microscale chemistry improvement engine: A pre-dosed microscale high-throughput experimentation additives platform enables rapid, serendipitous reaction improvement. This platform allowed one chemist to set up 475 experiments and analyze the results using MISER chromatography in a single day, thus resulting in two high-quality catalytic systems for the construction of the title compound 1. Support for a single-electron transfer mechanism was obtained. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：6912 / 6915

页数：4

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