L-751852

Chemical Name: 3-[4-(4-Methoxyphenyl)piperazin-1-ylmethyl]-1,4-dihydro-1H-benzopyrano[4,3-c]pyrazole
CAS No. 169155-54-8
项目整合开发状态: Preclinical
项目研究机构: Merck Sharp & Dohme (Originator)
合成路线:Condensation of 4-chromanone (I) with diethyl oxalate in the presence of sodium hexamethyldisilazane in THF at low temperature gave diketone (II),which on cyclization with hydrazine hydrochloride in refluxing ethanol provided pyrazole (III).Reduction of the ester group with LiAlH4 in THF yielded alcohol (IV).This was converted into chloride (V) by reaction with the complex between oxalyl chloride and dimethylformamide.Finally,alkylation of 1-(4-methoxyphenyl)piperazine (VI) with this chloride furnished the title compound.
📌 参考资料/链接:
参考文献标题:Fused tricyclic heteroaromatic derivs.as dopamine receptor subtype ligands
文献作者:Collins,I.J.; Leeson,P.D.; Rowley,M.(Merck Sharp & Dohme Ltd.)
参考来源:EP 0717733; JP 1997502199; WO 9507262