Methods for Selective Functionalization of (Hetero)arene Rings
(杂)芳烃环的选择性官能化方法
基本信息
- 批准号:10671746
- 负责人:
- 金额:$ 37.52万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2022
- 资助国家:美国
- 起止时间:2022-08-01 至 2027-05-31
- 项目状态:未结题
- 来源:
- 关键词:
项目摘要
Project Summary
This project aims to solve numerous challenges in aryne difunctionalization en route to highly decorated
arene rings, critical components of most pharmaceuticals. Currently, methods to functionalize arenes in multiple
positions require iterative coupling reactions. Difunctionalization of arynes provides an attractive strategy to
incorporate multiple functional groups into an arene ring. Unfortunately, these reactions are plagued with
problems with accessing starting materials due to multistep syntheses, limited reaction scope, and poor site
selectivity for the two possible positions of the triple bond in an aryne.
Our group aims to overcome all of these challenges by using transition metal catalysis to expand the
scope and utility of aryne difunctionalization. We plan to use C1 symmetric ligands in order to control
regioselectivity of the functional group addition to the aryne. Additionally, by the introduction of transition metal
catalysis with new aryne precursors that have previously never been used in catalysis, we will allow access to
aryne rings that were previously inaccessible due to ring strain. The transition metal catalyst will be able to bind
to the aryne and relieve ring strain. Finally, a wide variety of new difunctionalization reactions are proposed.
These new reactions encompass additions of F, N, and CF3 groups due to their importance in medicinal
chemistry.
If the goals of this proposal are achieved, we anticipate that this chemistry will provide easy access to a
wide variety of highly functionalized arene rings. These will provide important building blocks and opportunities
for late stage functionalization of medically relevant molecules.
项目摘要
该项目旨在解决芳炔双官能化过程中的众多挑战,以高度装饰
芳烃环是大多数药物的关键成分目前,在多个实施方案中官能化芳烃的方法是优选的。
位置需要反复的偶联反应。二官能化的arynes提供了一个有吸引力的策略,
将多个官能团引入芳烃环中。不幸的是,这些反应受到
由于多步合成、有限的反应范围和不良的场地,
芳炔中三键的两种可能位置的选择性。
我们小组的目标是克服所有这些挑战,通过使用过渡金属催化剂来扩大
芳炔双官能化的范围和效用。我们计划使用C1对称配体来控制
官能团加成到芳炔上的区域选择性。此外,通过引入过渡金属,
催化与新的芳炔前体,以前从未用于催化,我们将允许获得
芳炔环,以前由于环应变而不可接近。过渡金属催化剂将能够结合
芳炔并减轻环张力。最后,提出了各种新的双官能化反应。
这些新的反应包括添加F、N和CF3基团,因为它们在药物中的重要性。
化学.
如果这一提议的目标得以实现,我们预计这种化学反应将提供一种容易获得的方法,
各种高度官能化的芳烃环。这些将提供重要的基石和机会
用于医学相关分子的后期功能化。
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
数据更新时间:{{ journalArticles.updateTime }}
{{
item.title }}
{{ item.translation_title }}
- DOI:
{{ item.doi }} - 发表时间:
{{ item.publish_year }} - 期刊:
- 影响因子:{{ item.factor }}
- 作者:
{{ item.authors }} - 通讯作者:
{{ item.author }}
数据更新时间:{{ journalArticles.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ monograph.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ sciAawards.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ conferencePapers.updateTime }}
{{ item.title }}
- 作者:
{{ item.author }}
数据更新时间:{{ patent.updateTime }}
Courtney C Roberts其他文献
Courtney C Roberts的其他文献
{{
item.title }}
{{ item.translation_title }}
- DOI:
{{ item.doi }} - 发表时间:
{{ item.publish_year }} - 期刊:
- 影响因子:{{ item.factor }}
- 作者:
{{ item.authors }} - 通讯作者:
{{ item.author }}
相似国自然基金
不对称Tandem catalysis 合成手性仲醇
- 批准号:20643008
- 批准年份:2006
- 资助金额:8.0 万元
- 项目类别:专项基金项目
相似海外基金
Digital chemistry and catalysis: redefining reactions in confined systems
数字化学和催化:重新定义受限系统中的反应
- 批准号:
FL220100059 - 财政年份:2024
- 资助金额:
$ 37.52万 - 项目类别:
Australian Laureate Fellowships
"In-Crystallo" Solid-State Molecular Organometallic Chemistry of Methane, Ethane and Propane. Synthesis, Structures and Catalysis in Single-Crystals
甲烷、乙烷和丙烷的“晶体内”固态分子有机金属化学。
- 批准号:
EP/W015498/2 - 财政年份:2024
- 资助金额:
$ 37.52万 - 项目类别:
Research Grant
IonPairEnantRadical : Transforming Enantioselective Radical Chemistry using Ion Pairing Catalysis
IonPairEnantRadical:利用离子对催化转变对映选择性自由基化学
- 批准号:
EP/Y02348X/1 - 财政年份:2023
- 资助金额:
$ 37.52万 - 项目类别:
Research Grant
Multifunctional Peroxygenase Catalysis for Synthetic Chemistry
合成化学中的多功能过氧化酶催化
- 批准号:
EP/X014886/1 - 财政年份:2023
- 资助金额:
$ 37.52万 - 项目类别:
Research Grant
Computational prediction of hot-electron chemistry: Towards electronic control of catalysis
热电子化学的计算预测:迈向催化的电子控制
- 批准号:
MR/X023109/1 - 财政年份:2023
- 资助金额:
$ 37.52万 - 项目类别:
Fellowship
Catalysis, Reactivity and Probe Development in Carbohydrate-Based Chemistry and Biochemistry
碳水化合物化学和生物化学中的催化、反应性和探针开发
- 批准号:
RGPIN-2017-04910 - 财政年份:2022
- 资助金额:
$ 37.52万 - 项目类别:
Discovery Grants Program - Individual
Boron Chemistry for Catalysis and Drug Discovery
用于催化和药物发现的硼化学
- 批准号:
CRC-2015-00074 - 财政年份:2022
- 资助金额:
$ 37.52万 - 项目类别:
Canada Research Chairs
"In-Crystallo" Solid-State Molecular Organometallic Chemistry of Methane, Ethane and Propane. Synthesis, Structures and Catalysis in Single-Crystals
甲烷、乙烷和丙烷的“晶体内”固态分子有机金属化学。
- 批准号:
EP/W015498/1 - 财政年份:2022
- 资助金额:
$ 37.52万 - 项目类别:
Research Grant
"In-Crystallo" Solid-State Molecular Organometallic Chemistry of Methane, Ethane and Propane. Synthesis, Structures and Catalysis in Single-Crystals
甲烷、乙烷和丙烷的“晶体内”固态分子有机金属化学。
- 批准号:
EP/W015552/1 - 财政年份:2022
- 资助金额:
$ 37.52万 - 项目类别:
Research Grant
Organometallic Chemistry of the Nonmetals: Unlocking New Approaches to Green Catalysis
非金属有机金属化学:开辟绿色催化新方法
- 批准号:
RGPIN-2021-03814 - 财政年份:2022
- 资助金额:
$ 37.52万 - 项目类别:
Discovery Grants Program - Individual