Meclinertant, Reminertant, SR-48692-药物合成数据库

【药物名称】Meclinertant, Reminertant, SR-48692

化学结构式(Chemical Structure):

参考文献No.	17213
标题:	Amido-3-pyrazole derivs., process for their preparation and pharmaceutical compsns. containing them
作者:	Boigegrain, R.; Gully, D.; Jeanjean, F.; Molimard, J.-C. (Sanofi-Synth閘abo )
来源:	EP 0477049; FR 2665898; JP 1992244065; US 5420141; US 5607958; US 5616592; US 5635526; US 5744491; US 5744493

合成路线图解说明: The condensation of 2',6'-dimethoxyacetophenone (I) with diethyl oxalate (II) by means of sodium methoxide in refluxing methanol gives the dioxobutyrate (III), which is cyclized with 7-chloroquinoline-4-hydrazine (IV) in refluxing acetic acid yielding the pyrazole derivative (V). The hydrolysis of the ester group of (V) with KOH in refluxing methanol/water affords the corresponding carboxylic acid (VI), which is finally treated with SOCl2 in refluxing toluene and condensed with 2-aminoadamantane-2-carboxylic acid.

参考文献No.	233925
标题:	Neurotensin receptor agonists and antagonists
作者:	Maffrand, J.P.; Gully, D.; Boigegrain, R.; Soubrie, P.; Kitabgi, P.; Rostene, W.; Le Fur, G.
来源:	Drugs Fut 1993,18(12),1137

合成路线图解说明: The condensation of 2',6'-dimethoxyacetophenone (I) with diethyl oxalate (II) by means of sodium methoxide in refluxing methanol gives the dioxobutyrate (III), which is cyclized with 7-chloroquinoline-4-hydrazine (IV) in refluxing acetic acid yielding the pyrazole derivative (V). The hydrolysis of the ester group of (V) with KOH in refluxing methanol/water affords the corresponding carboxylic acid (VI), which is finally treated with SOCl2 in refluxing toluene and condensed with 2-aminoadamantane-2-carboxylic acid.