On June 6, 1996, Achard, Daniel; Peyronel, Jean-Francois; Tabart, Michel published a patent.Formula: C10H12O3 The title of the patent was Perhydroisoindole derivatives as antagonists of substance p. And the patent contained the following:
New perhydroinsoindoles having the general formula I wherein R1 is optionally substituted Ph or is cyclohexadienyl, naphthyl, indenyl or mono or polycyclic heterocyclyl, saturated or unsaturated 5 to 9C and optionally substituted, R2 is H or halogen, OH, alkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkyloxy, alkylthio, acyloxy, carboxy, alkyloxycarbonyl, dialkylaminoalcyloxycarbonyl, benzyloxycarbonyl, amino or acylamino, R3 is Ph optionally substituted in position -2 by a radical alkyl or alkyloxy 1 or 2C or by OH or F, or disubstituted by CF3, and R4 is an alkyl radical containing 1 or 2C substituted by halogen or CN, N3 or -NHCN, and the radicals R which are similar or different represent H, alkyl or Ph, in their isomer forms having the structure II or mixtures thereof, optionally their salts when they exist and preparation thereof. The new derivatives of the invention are particularly useful as antagonists of substance P. The derivative II (R = H, R1 = Me, R2 = R3 = 2-MeOC6H4, R4 = CH2OH) was prepared via acylation of (卤)-III with (S)-(2-MeOC6H4)CHMeCO2H in CH2Cl2 containing hydroxybenzotriazole hydrate and EtN:C:N(CH2)3NMe2. The antiinflammatory activity of several II were tested with a DE50 mg/kg p.o. range of 0.004-1. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Formula: C10H12O3
The Article related to substance p antagonist preparation, perhydroisoindole derivative preparation bioactivity, isoindole perhydro derivative preparation bioactivity, nk2 receptor antagonist preparation and other aspects.Formula: C10H12O3
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