Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling Reactions
在交叉偶联反应中利用烷基胺和烷基醇
基本信息
- 批准号:10617925
- 负责人:
- 金额:$ 5.97万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2019
- 资助国家:美国
- 起止时间:2019-06-01 至 2024-05-31
- 项目状态:已结题
- 来源:
- 关键词:3-DimensionalAddressAlcoholsAminesAwarenessCarbonChemistryComplexCouplingDevelopmentGoalsMedicineMethodsNickelNitrogenOxidation-ReductionOxygenPharmaceutical PreparationsPreparationPublic HealthReactionReagentResearchSaltsdrug developmentfunctional grouphuman diseaseinventionnovel therapeuticsprograms
项目摘要
The search for new medicines requires the discovery of new molecules, and the increasing awareness that
saturated atoms correlate to successful drug development mandates that these molecules be three-
dimensional. This increasing importance of saturated carbons in bioactive molecules provides exciting
opportunities for the invention of new cross-coupling methods and new alkyl electrophiles from widely
abundant starting materials. This research will focus on alkyl alcohols and amines for their unique and exciting
potential as cross-coupling electrophiles. Alkyl amines and alcohols have traditionally been seen as synthetic
targets, not substrates. However, their wide availability and the ease of their preparation in highly
enantioenriched form makes them attractive alkyl electrophiles to address challenges in asymmetric synthesis
and to identify new, previously untapped feedstocks for synthesis.
Alkyl amines and alcohols can be prepared in high enantiopurity, making them ideal substrates for
stereospecific cross-coupling reactions. Via carbon–oxygen (C–O) and carbon–nitrogen (C–N) bond cleavage
of highly enantioenriched alcohol and amine derivatives, we will solve longstanding challenges in asymmetric
synthesis. These stereospecific cross-couplings will advance these alcohol and amine intermediates into
valuable, highly enantioenriched products, including those with traditionally challenging all-carbon quaternary
stereocenters.
Primary alkyl amines are found in molecules ranging from simple starting materials to drugs and
biomolecules. Harnessing the ubiquitous amino (NH2) group, this research will develop chemistry to transform
NH2 groups into a host of other functional groups via cleavage of the C–N bond. The ability to transform a C–N
bond to a C–C (or C–X) bond offers powerful opportunities in late-stage functionalization of complex alkyl
amines, derivatization of biomolecules, and early-stage synthesis. This goal will be accomplished via nickel-
catalyzed cross couplings of redox-active Katritzky pyridinium salts, which are readily and selectively prepared
from primary alkyl amines.
The successful development of this chemistry will enable efficient access to three-dimensional molecules
with potential bioactivity from widely available precursors. This research will also change the way chemists see
and use these functional groups. The ultimate goal of this research is to invent cross-coupling methods for
C(sp3)–X electrophiles that are as useful as those long-known for C(sp2)–X reagents for the discovery and
synthesis of new medicines. By opening a new door for the synthesis of novel, drug-like molecules, this
research will impact the discovery of new molecules with the potential to deepen our understanding of and
ability to treat human disease.
寻找新药需要发现新的分子,并日益意识到
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 }}
Mary P Watson其他文献
Empowering Women in Organic Chemistry (EWOC) at Five Years: Giving Back and Getting Back.
五年内赋予女性有机化学 (EWOC) 权力:回馈与回报。
- DOI:
10.1021/acs.jmedchem.3c01704 - 发表时间:
2023 - 期刊:
- 影响因子:7.3
- 作者:
Elinor H Cantor;M. Faul;Donna M. Huryn;Lara Kallander;Rebecca T. Ruck;Mary P Watson - 通讯作者:
Mary P Watson
Mary P Watson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('Mary P Watson', 18)}}的其他基金
Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling Reactions
在交叉偶联反应中利用烷基胺和烷基醇
- 批准号:
10728392 - 财政年份:2019
- 资助金额:
$ 5.97万 - 项目类别:
Supplement to Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling
在交叉偶联中利用烷基胺和烷基醇的补充
- 批准号:
10436560 - 财政年份:2019
- 资助金额:
$ 5.97万 - 项目类别:
Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling Reactions
在交叉偶联反应中利用烷基胺和烷基醇
- 批准号:
10412949 - 财政年份:2019
- 资助金额:
$ 5.97万 - 项目类别:
Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling Reactions
在交叉偶联反应中利用烷基胺和烷基醇
- 批准号:
10166874 - 财政年份:2019
- 资助金额:
$ 5.97万 - 项目类别:
Administrative Supplement to Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling
在交叉偶联中利用烷基胺和烷基醇的行政补充
- 批准号:
10798396 - 财政年份:2019
- 资助金额:
$ 5.97万 - 项目类别:
Harnessing Alkyl Amines and Alkyl Alcohols in Cross-Coupling Reactions
在交叉偶联反应中利用烷基胺和烷基醇
- 批准号:
10620171 - 财政年份:2019
- 资助金额:
$ 5.97万 - 项目类别:
Cross Couplings of Amine and Alcohol Derivatives to Give Enantioenriched Products
胺和醇衍生物的交叉偶联产生对映体富集的产品
- 批准号:
8766156 - 财政年份:2014
- 资助金额:
$ 5.97万 - 项目类别:
Cross Couplings of Amine and Alcohol Derivatives to Give Enantioenriched Products
胺和醇衍生物的交叉偶联产生对映体富集的产品
- 批准号:
9021912 - 财政年份:2014
- 资助金额:
$ 5.97万 - 项目类别:
Catalytic, Asymmetric Aziridination using (Salen)metal Catalysts
使用 (Salen) 金属催化剂进行催化不对称氮丙啶化
- 批准号:
7383897 - 财政年份:2007
- 资助金额:
$ 5.97万 - 项目类别:
Catalytic, Asymmetric Aziridination using (Salen)metal Catalysts
使用 (Salen) 金属催化剂进行催化不对称氮丙啶化
- 批准号:
7275202 - 财政年份:2007
- 资助金额:
$ 5.97万 - 项目类别:
相似海外基金
Rational design of rapidly translatable, highly antigenic and novel recombinant immunogens to address deficiencies of current snakebite treatments
合理设计可快速翻译、高抗原性和新型重组免疫原,以解决当前蛇咬伤治疗的缺陷
- 批准号:
MR/S03398X/2 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Fellowship
Re-thinking drug nanocrystals as highly loaded vectors to address key unmet therapeutic challenges
重新思考药物纳米晶体作为高负载载体以解决关键的未满足的治疗挑战
- 批准号:
EP/Y001486/1 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Research Grant
CAREER: FEAST (Food Ecosystems And circularity for Sustainable Transformation) framework to address Hidden Hunger
职业:FEAST(食品生态系统和可持续转型循环)框架解决隐性饥饿
- 批准号:
2338423 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Continuing Grant
Metrology to address ion suppression in multimodal mass spectrometry imaging with application in oncology
计量学解决多模态质谱成像中的离子抑制问题及其在肿瘤学中的应用
- 批准号:
MR/X03657X/1 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Fellowship
CRII: SHF: A Novel Address Translation Architecture for Virtualized Clouds
CRII:SHF:一种用于虚拟化云的新型地址转换架构
- 批准号:
2348066 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Standard Grant
BIORETS: Convergence Research Experiences for Teachers in Synthetic and Systems Biology to Address Challenges in Food, Health, Energy, and Environment
BIORETS:合成和系统生物学教师的融合研究经验,以应对食品、健康、能源和环境方面的挑战
- 批准号:
2341402 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Standard Grant
The Abundance Project: Enhancing Cultural & Green Inclusion in Social Prescribing in Southwest London to Address Ethnic Inequalities in Mental Health
丰富项目:增强文化
- 批准号:
AH/Z505481/1 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Research Grant
ERAMET - Ecosystem for rapid adoption of modelling and simulation METhods to address regulatory needs in the development of orphan and paediatric medicines
ERAMET - 快速采用建模和模拟方法的生态系统,以满足孤儿药和儿科药物开发中的监管需求
- 批准号:
10107647 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
EU-Funded
Ecosystem for rapid adoption of modelling and simulation METhods to address regulatory needs in the development of orphan and paediatric medicines
快速采用建模和模拟方法的生态系统,以满足孤儿药和儿科药物开发中的监管需求
- 批准号:
10106221 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
EU-Funded
Recite: Building Research by Communities to Address Inequities through Expression
背诵:社区开展研究,通过表达解决不平等问题
- 批准号:
AH/Z505341/1 - 财政年份:2024
- 资助金额:
$ 5.97万 - 项目类别:
Research Grant