烯胺酰化/缩合一锅法构建5,6,7,8-四氢吡啶[4,3-d]嘧啶核心结构及其在5HT_(2A)受体拮抗剂合成上的应用(英文)
A One-pot Enamine Acylation/Condensation Sequence to Construct 5,6,7,8-Tetrahydropyrido[4,3-d]pyrimidine:An Efficient Synthesis of a Selective 5HT_(2A) Receptor Antagonist
摘要
报道了1条5HT_(2A)受体拮抗剂的高选择性合成路线.烯胺酰化/缩合一锅法可用于有效构建5,6,7,8-四氢吡啶[4,3-d]嘧啶核心结构,其中哌啶催化剂的使用对于这一新方法至关重要.
We have developed a highly efficient synthesis of compound 1, a sel.ective 5HT2A receptor antagonist, featuring a one-pot enamine acylation/cyclization protocol to construct the 5, 6, 7, 8-tetrahydropyrido [4, 3-d] pyrimidine core structure. Piperidine as the secondary amine catalyst of choice is crucial for the success of this new procedure.
出处
《复旦学报（自然科学版）》
CAS
CSCD
北大核心
2012年第5期637-643,共7页
Journal of Fudan University：Natural Science
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