Exploiting Unconventional Building Blocks in Chemical Synthesis
在化学合成中利用非常规构件
基本信息
- 批准号:10330994
- 负责人:
- 金额:$ 58.23万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2021
- 资助国家:美国
- 起止时间:2021-02-01 至 2026-01-31
- 项目状态:未结题
- 来源:
- 关键词:
项目摘要
Project Summary/Abstract
The central objective of this application is to harness unconventional synthetic
building blocks for the development of new, reliable, and efficient, methodologies.
These methodologies are intended to enable the construction of stereochemically rich
scaffolds, including those seen in naturally occurring small molecules and medicines.
The development of new methods and the syntheses of complex small molecules
continues to be vital areas of research. Most medicinal agents on the market are
prepared by organic synthesis, including the large majority of all new drugs that have
become available over the past three decades. The chemical structures of new drug
entities are becoming increasingly complex, now often bearing sp3 centers rather than
“flat” structures. This has led to an increased need for chemists to develop new
methods that can reliably build intricate structures.
The two unconventional building blocks we seek to harness in the proposed
studies are amides and strained cyclic alkynes and allenes. Regarding amides, the C–N
bond of amides has long been viewed as stable, such that synthetic methodologies that
rely on C–N bond cleavage have remained limited. We seek to develop methods that
utilize nickel catalysis to harness amide functional groups as synthons. We propose to
assemble important linkages with defined stereocenters, including quaternary
stereocenters, using catalysis and chemoenzymatic methods. These efforts provide
new opportunities in the area of strong bond activation by nickel catalysis, along with
new tools for the manipulation of amides via C–N bond cleavage. With regard to
strained cyclic alkynes and allenes, we seek to intercept these transient, highly reactive
species to efficiently build complex molecular scaffolds. Such methods should allow for
the establishment of scaffolds bearing two new bonds and three sp3 centers.
Enantiospecific and catalytic enantioselective variants will be targeted. Our
methodologies will be evaluated in the context of several synthetic endeavors. The
results of our studies should lead to powerful new strategies and tools for accessing
various molecules of importance, including natural products and medicines.
项目摘要/摘要
这一应用的中心目标是利用非传统的合成
构建开发新的、可靠和高效的方法的基础。
这些方法旨在使立体化学富集物的构建成为可能
支架,包括那些自然产生的小分子和药物中的支架。
新方法的发展与复杂小分子的合成
仍然是重要的研究领域。市场上的大多数药物都是
由有机合成制成,包括绝大多数具有
在过去的三十年里可以使用。新药的化学结构
实体正变得越来越复杂,现在通常带有SP3中心,而不是
“扁平”结构。这导致了对化学家开发新的
可以可靠地构建复杂结构的方法。
我们希望在拟议的
研究的是酰胺和张力环炔和烯。关于酰胺,C-N
长期以来,酰胺键一直被认为是稳定的,因此合成方法
依赖C-N键裂解的情况仍然有限。我们寻求开发出方法,
利用镍催化来利用酰胺官能团作为合成子。我们建议
通过定义的立体中心(包括第四级)组装重要的链接
立体中心,使用催化和化学酶方法。这些努力提供了
镍催化强键活化领域的新机遇,以及
通过C-N键裂解来操纵酰胺的新工具。关于……
张力环炔和烯,我们试图截获这些瞬变的,高活性的
物种高效地构建复杂的分子支架。这种方法应该允许
建立了承载两个新键和三个SP3中心的支架。
对映异构体和催化对映体选择性变异体将成为靶标。我们的
方法论将在几项综合努力的背景下进行评估。这个
我们的研究结果应该会带来强大的新战略和工具,以获取
各种重要的分子,包括天然产品和药物。
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 }}
NEIL K GARG其他文献
NEIL K GARG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 }}
{{ truncateString('NEIL K GARG', 18)}}的其他基金
NMR Console and Prodigy CryoProbe
NMR 控制台和 Prodigy CryoProbe
- 批准号:
10177110 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Exploiting Unconventional Building Blocks in Chemical Synthesis
在化学合成中利用非常规构件
- 批准号:
10559768 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Exploiting Unconventional Building Blocks in Chemical Synthesis
在化学合成中利用非常规构件
- 批准号:
10727713 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Exploiting Unconventional Building Blocks in Chemical Synthesis
在化学合成中利用非常规构件
- 批准号:
10399170 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Exploiting Unconventional Building Blocks in Chemical Synthesis
在化学合成中利用非常规构件
- 批准号:
10560628 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Biosynthesis and Enzymology of Antifungal Natural Products
抗真菌天然产物的生物合成和酶学
- 批准号:
10513326 - 财政年份:2018
- 资助金额:
$ 58.23万 - 项目类别:
Biosynthesis and Enzymology of Antifungal Natural Products
抗真菌天然产物的生物合成和酶学
- 批准号:
10291416 - 财政年份:2018
- 资助金额:
$ 58.23万 - 项目类别:
Biosynthesis and Enzymology of Antifungal Natural Products
抗真菌天然产物的生物合成和酶学
- 批准号:
10066257 - 财政年份:2018
- 资助金额:
$ 58.23万 - 项目类别:
Harnessing Strained Intermediates to Access Complex Molecules
利用应变中间体访问复杂分子
- 批准号:
9523411 - 财政年份:2018
- 资助金额:
$ 58.23万 - 项目类别:
New Directions in Cross-Couplings Catalyzed by Non-Precious Metals
非贵金属催化交叉偶联的新方向
- 批准号:
9892311 - 财政年份:2016
- 资助金额:
$ 58.23万 - 项目类别:
相似海外基金
Collaborative Research: NSF-DFG: CAS: Electrochemical Hydrogenation of Amides and Esters
合作研究:NSF-DFG:CAS:酰胺和酯的电化学氢化
- 批准号:
2140205 - 财政年份:2022
- 资助金额:
$ 58.23万 - 项目类别:
Standard Grant
Collaborative Research: NSF-DFG: CAS: Electrochemical Hydrogenation of Amides and Esters
合作研究:NSF-DFG:CAS:酰胺和酯的电化学氢化
- 批准号:
2140196 - 财政年份:2022
- 资助金额:
$ 58.23万 - 项目类别:
Standard Grant
Atroposelective Synthesis of Hindered Amides - Exploration of Synthetic Peptide Catalysts -
受阻酰胺的天体选择性合成-合成肽催化剂的探索-
- 批准号:
504378162 - 财政年份:2022
- 资助金额:
$ 58.23万 - 项目类别:
WBP Fellowship
Development of Peptide Chemical Modification Enabled by N-Halogenation of Amides
酰胺 N-卤化实现的肽化学修饰的发展
- 批准号:
22H02743 - 财政年份:2022
- 资助金额:
$ 58.23万 - 项目类别:
Grant-in-Aid for Scientific Research (B)
Modulating Signaling Endocannabinoids and Fatty Acid Amides
调节信号传导内源性大麻素和脂肪酸酰胺
- 批准号:
10532252 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
CAREER: SusChEM: Iron Catalysts for the Reduction of Amides
职业:SusChEM:用于还原酰胺的铁催化剂
- 批准号:
2146728 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Continuing Grant
Modulating Signaling Endocannabinoids and Fatty Acid Amides
调节信号传导内源性大麻素和脂肪酸酰胺
- 批准号:
10399712 - 财政年份:2021
- 资助金额:
$ 58.23万 - 项目类别:
Function of primary fatty acid amides as lipid mediators
伯脂肪酸酰胺作为脂质介质的功能
- 批准号:
20K21285 - 财政年份:2020
- 资助金额:
$ 58.23万 - 项目类别:
Grant-in-Aid for Challenging Research (Exploratory)
Nickel-Catalyzed Alpha-Arylation of Secondary Amides
镍催化仲酰胺的α-芳基化
- 批准号:
558383-2020 - 财政年份:2020
- 资助金额:
$ 58.23万 - 项目类别:
Canadian Graduate Scholarships Foreign Study Supplements
Catalytic Synthesis of Pharmaceutical Amides in Water
水中催化合成药用酰胺
- 批准号:
EP/T01430X/1 - 财政年份:2020
- 资助金额:
$ 58.23万 - 项目类别:
Research Grant