Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery

被引：17
|
作者：
Geary, Gemma C. [1 ]
Nortcliffe, Andrew [1 ]
Pearce, Christopher A. [2 ]
Hamza, Daniel [2 ]
Jones, Geraint [2 ]
Moody, Christopher J. [1 ]
机构：
[1] Univ Nottingham, Sch Chem, Univ Pk, Nottingham NG7 2RD, England
[2] Sygnature Discovery Ltd, BioCity, Pennyfoot St, Nottingham NG1 1GF, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2018年 / 26卷 / 04期
关键词：
LEAD-ORIENTED SYNTHESIS; CHEMISTRY;
D O I：
10.1016/j.bmc.2017.12.012
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A spirocyclic, sp(3)-atom rich oxetane-containing scaffold was synthesised in just two steps via a gold catalysed propargylic alcohol rearrangement. The key gold cyclisation can be undertaken on a 40 g scale allowing the preparation of 419 lead-like compounds based on the scaffold for the European Lead Factory. (C) 2017 Elsevier Ltd. All rights reserved.
引用
收藏
页码：791 / 797
页数：7
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