SYNTHESIS & SYNTHETIC UTILITY OF 1-ACYLDIHYDROPYRIDINES

合成

• 批准号: 3285444
• 负责人: DANIEL L COMINS
• 金额: $ 14.86万
• 依托单位: NORTH CAROLINA STATE UNIVERSITY RALEIGH
• 依托单位国家: 美国
• 财政年份: 1989
• 资助国家: 美国
• 起止时间: 1989-01-01 至 1995-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3285444
• 关键词: Diels Alder reaction; acylation; alkaloids; alkylation; chemical synthesis; dihydropyridines; halocarbon compound; halogenation; heterocyclic compounds; indolizines; organometallic compounds; quinolizine; stereoisomer

The objective of this proposal is to develop methods for the synthesis of novel 1-acyldihydropyridines and to study their utility as synthetic intermediates. Specific aims are (1) To study the asymmetric synthesis of 1-acyl-2-alkyl-1,2-dihydropyridines and 2-alkyl-2, 3-dihydro- 4 - pyridones. (2) To investigate the asymmetric synthesis and synthetic utility of 1-acyl-2-triphenylsilyl-2,3-dihydro-4-pyridones. (3) To develop enantioselective syntheses of various indolizidine and quinolizidine alkaloids using homochiral 2,3-dihydro-4-pyridones as synthetic intermediates. The proposed methodology will be useful for tbe synthesis of compounds having a broad range of biological properties, i.e. neuroleptic, antihypertensive, antiinflamatory, antitumor, and anticonvulsant activities.

这项提议的目标是开发合成方法。 新型1-酰基二氢吡啶的合成及其应用研究 中间体。具体目标是：(1)研究不对称合成 1-酰基-2-烷基-1，2-二氢吡啶和2-烷基-2，3-二氢-4- 吡喃酮类化合物。(2)研究了不对称合成和合成 1-acyl-2-triphenylsilyl-2，3-dihydro-4-pyridones.的实用性(3)至 开发不对称合成各种吲哚里西定和 以高手性2，3-二氢-4-吡啶酮为原料的喹啉类生物碱 合成中间体。 所提出的方法对化合物的合成有一定的参考价值。 具有广泛的生物学特性，即抗精神病药物， 抗高血压、抗炎、抗肿瘤、抗惊厥 活动。