摘要
以 6 硝基胡椒醛为原料 ,经亲核氟化、还原碘化、手性相转移催化对映选择烷基化及水解等多步反应合成 6 氟 L 多巴 ,总产率约为 38%。用手性流动相结合反相C18柱的HPLC法测定 6 氟 L 多巴的对映纯度大于 95 %。
Fluoro-L-DOPA was synthesized from the starting material 6-nitropiperonal via a multi-step reaction by the nucleophilic fluorination,reductive iodination,chiral catalytic phase-transfer alkylation,and hydrolysis reactions.The enantiomeric purity of 6-fluoro-L-DOPA was determined by the HPLC method using a chiral mobile phase and reversed-phase C 18 column.The overall chemical yield from 6-nitropiperonal was 38%,and the enantiomeric purity of 6-fluoro-L-DOPA was above 95%.
出处
《中国药物化学杂志》
CAS
CSCD
2002年第1期39-42,共4页
Chinese Journal of Medicinal Chemistry
基金
"九五"国家重点科技项目 (攻关 )计划 (96 -B12 - 0 4- 0 2 - 2 )
中国博士后科学基金项目
广东省自然科学基金项目 (0 0 110 4)
