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

页码：791 / 797

页数：7

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