SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES AND PROSTA
生物活性杂环和前列腺素的合成
基本信息
- 批准号:3272150
- 负责人:
- 金额:$ 13.87万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:1977
- 资助国家:美国
- 起止时间:1977-09-01 至 1986-08-31
- 项目状态:已结题
- 来源:
- 关键词:alpha benzopyrone antibiotics antifungal agents benzodiazepines benzofurans beta lactam antibiotic carbonyl compound cardiovascular disorder chemotherapy drug design /synthesis /production furans heterocyclic compounds indoles isoquinolines lactams lactones mercury palladium pyrroles quinoline reproductive system disorder chemotherapy saturated /unsaturated bonds thallium
项目摘要
A number of potentially important new synthetic routes to heterocyclic
compounds, including furans, butenolides, benzofurans, chromenes,
coumarins, isocoumarins, Beta-lactams, tetramic acids, pyrroles, indoles,
quinolines, isoquinolines and benzodiazepines, are outlined. These
heterocycles occur widely in nature and exhibit substantial physiological
activity. They have found use in the treatment of cancer, circulatory and
heart ailments, and bacterial and fungal infections. A broad spectrum of
antibiotic activity is evident among these compounds. Our previous work on
new synthetic applications of organometallic compounds has suggested a
number of novel new approaches to these ring systems, all of which take
advantage of the ease with which organopalladium compounds can be prepared
from either organomercury or -thallium compounds or via direct palladation
of acetylenes and aromatic compounds, and the facility with which
organopalladium compounds react with carbon monoxide or olefins to generate
new carbon-carbon bonds. The appropriate positioning of functional groups
should allow novel new syntheses of the heterocyclic ring systems mentioned
above. Successful completion of this work shold (1) open up entirely new
routes to these naturally occurring, biologically active heterocycles, (2)
provide a number of interesting new compounds which might be expected to
show physiological activity and hopefully medicinal utility, and finally
(3) simplify many a synthesis of these vitally important heterocycles.
许多潜在重要的杂环新合成路线
化合物,包括呋喃,丁烯内酯,苯并呋喃,色烯,
香豆素、异香豆素、β-内酰胺、特特拉姆酸、吡咯、吲哚,
喹啉、异喹啉和苯并二氮杂。 这些
杂环广泛存在于自然界中,并表现出显著的生理活性
活动 它们已被发现用于治疗癌症、循环系统疾病和
心脏病,细菌和真菌感染。 广泛的
在这些化合物中,抗生素活性是明显的。 我们以前的工作
有机金属化合物的新的合成应用已经提出了一个
许多新颖的新方法,这些环系统,所有这些都需要
有机钯化合物易于制备的优点
从有机汞或铊化合物或通过直接钯化
乙炔和芳香族化合物,和设施,
有机钯化合物与一氧化碳或烯烃反应,
新的碳碳键 职能组的适当定位
应该允许新的新的合成所提到的杂环系统
以上 这项工作的顺利完成,应(1)开辟全新的
这些天然存在的、具有生物活性的杂环的途径,(2)
提供了许多有趣的新化合物,预计这些化合物可能会
显示出生理活性和希望的药用价值,
(3)简化了这些极其重要杂环的许多合成。
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)
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RICHARD C. LAROCK其他文献
RICHARD C. LAROCK的其他文献
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{{ truncateString('RICHARD C. LAROCK', 18)}}的其他基金
Heterocyclic /Carbocyclic Libraries for High Throughput
高通量杂环/碳环文库
- 批准号:
7193848 - 财政年份:2006
- 资助金额:
$ 13.87万 - 项目类别:
Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
用于高通量筛选的中试规模杂环和碳环文库
- 批准号:
7286748 - 财政年份:2006
- 资助金额:
$ 13.87万 - 项目类别:
Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
用于高通量筛选的中试规模杂环和碳环文库
- 批准号:
7925143 - 财政年份:2006
- 资助金额:
$ 13.87万 - 项目类别:
Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
用于高通量筛选的中试规模杂环和碳环文库
- 批准号:
7487400 - 财政年份:2006
- 资助金额:
$ 13.87万 - 项目类别:
Synthesis of Medicinally Important Heterocycles
具有药用价值的杂环化合物的合成
- 批准号:
7121537 - 财政年份:2004
- 资助金额:
$ 13.87万 - 项目类别:
Synthesis of Medicinally Important Heterocycles
具有药用价值的杂环化合物的合成
- 批准号:
6945402 - 财政年份:2004
- 资助金额:
$ 13.87万 - 项目类别:
Synthesis of Medicinally Important Heterocycles
具有药用价值的杂环化合物的合成
- 批准号:
7282502 - 财政年份:2004
- 资助金额:
$ 13.87万 - 项目类别:
Synthesis of Medicinally Important Heterocycles
具有药用价值的杂环化合物的合成
- 批准号:
6759066 - 财政年份:2004
- 资助金额:
$ 13.87万 - 项目类别:
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