On June 5, 1991, Dubroeucq, Marie Christine; Moutonnier, Claude; Peyronel, Jean Francois; Tabart, Michel; Truchon, Alain published a patent.Category: ethers-buliding-blocks The title of the patent was Isoindolone derivatives, useful as intermediates for substance P antagonists, and their preparation. And the patent contained the following:
Title compounds I [both R = H; or RR = bond; R1 = H, easily removed radical; R2 = (identically) Ph substituted optionally by halo or Me in ortho or meta position] (II), especially the (3aRS,7aRS)- and (3aR,7aR)-isomers, are prepared as intermediates for I [R1 = C(X)CHR3R4; X = O, S, NR5; R3 = (substituted) Ph, cyclohexadienyl, naphthyl, heterocyclyl; R4 = H, halo, OH, alkyl, aminoalyl, alkoxy, CO2H, amino, etc.; R5 = H, (substituted) alkyl, dialkylamino] (III), which are antagonists of substance P (no data) were prepared Cyclocondensation of 4,4-diphenyl-2-cyclohexen-1-one with PhCH2N(CH2OBu)CH2SiMe3 in CH2Cl2 in the presence of CF3CO2H gave (3aRS,7aRS)-I (R = H, R1 = CH2Ph, R2 = Ph); this was debenzylated by H over Pd/C in MeOH-HCl and the product (R2 = H) amidated by PhCH2CO2H using N,N’-carbonyldiimidazole and Et3N in CH2Cl2 to give (3aRS,7aRS)-I (R = H, R1 = COCH2Ph, R2 = Ph). Seventeen syntheses of II and 24 of III are described. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Category: ethers-buliding-blocks
The Article related to isoindolone intermediate substance p antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: ethers-buliding-blocks
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Ether | (C2H5)2O – PubChem