Crespo, Andre et al. published their patent in 1994 |CAS: 81616-80-0

The Article related to arylperhydroisoindolediol preparation neurokinin antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 81616-80-0

On October 13, 1994, Crespo, Andre; Fardin, Veronique; Guillaume, Jean-Marc; Malleron, Jean -Luc; Peyronel, Jean-Francois published a patent.Application of 81616-80-0 The title of the patent was Preparation of pharmaceutical perhydroisoindole derivatives as neurokinin A antagonists. And the patent contained the following:

Title compounds I (R = (substituted)Ph; R1 = (substituted)Ph, PhCh2O, (substituted)-C1-4 alkyl, (substituted)amino, (substituted)heterocyclyl, cyclohexadienyl, naphthyl, indenyl; R2 = H, halo, HO, alkyl, aminoalkyl, allylaminoalkyl, dialkylaminoalkyl, etc.; R3 = (substituted)Ph), are prepared (3AR,4R,5R,7aR)-7,7-diphenyl-4-(2-methoxyphenyl)perhydro-4,5-isoindolediol (preparation given) and 3-indolylacetic acid in CH2Cl2 were added to 1-benzotriazolylol hydrate, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and diisopropylethylamine to give (3aR,4R,5R,7aR)-I (R1 = 3-indolyl, R2 = H, R3 – 2-(MeO)C6H4) which at 10-1000 nM on human receptor NK2 showed IC50 of 215 nM. A formulation tablet comprising I is given. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).Application of 81616-80-0

The Article related to arylperhydroisoindolediol preparation neurokinin antagonist, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Application of 81616-80-0

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem