摘要
研究了2'-羟基查耳酮的Mannich反应,发现该反应区域选择性地发生在查耳酮B环C-3'位,利用此法共合成了12个新的Mannich碱化合物,其结构经元素分析、1HNMR和IR得到确证.该反应制备步骤简单,条件温和,产物易纯化,收率从中等到高(49～72%).初步的生物活性测定表明其中部分化合物具强效的CDK1/cyclinB抑制活性,多数化合物对肿瘤细胞具较强的抑制活性.
Twelve Mannich base derivatives of 2＇-hydroxychalcone were synthesized through Mannich reaction, and the regioselectivity of the reaction occurred preferentially at C-3＇ position of B ring of chalcone backbone. All the target compounds have been identified by ^1H NMR, IR spectra and elemental analyses, and further confirmed by X-ray analysis. The characteristic of this reaction was simple process, mild condition, easy purification and middle to good yields （49% ～ 72%）. Some compounds showed potent CDK1/cyclin B inhibitory activities and most of compounds displayed a significant growth inhibitory action against various cancer cell lines.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2006年第7期983-987,共5页
Chinese Journal of Organic Chemistry
