On January 17, 1997, Commercon, Alain; Lebrun, Alain; Mailliet, Patrick; Peyronel, Jean Francois; Sounigo, Fabienne; Truchon, Alain; Zucco, Martine; Cheve, Michel published a patent.SDS of cas: 81616-80-0 The title of the patent was New benzisoindole derivatives as inhibitors of farnesyl transferase, their preparation, and pharmaceutical compositions containing them.. And the patent contained the following:
Title compounds I [R = (un)substituted (CH2)mX1(CH2)nZ; X1 = bond, O, S; m = 0-1; n = 0-2; Z = CO2H, alkoxycarbonyl, (un)substituted carbamoyl, etc.; R1, R2 = H, halo, alkyl, (un)substituted alkoxy; or R1R2 form (un)saturated heterocycle; or R2 forms dimer via disulfide bridge; R3 = H, halo, alkyl, alkenyl, alkoxy, alkylthio; X = O, S, NH, CO, CH2, CH2CH2, alkylene, 1,1-cycloalkanediyl; Y = O, S], in racemic form or as optical isomers, are claimed. The compounds are inhibitors of farnesyl transferase, and show marked antitumor and antileukemic properties. For example, cis-3,6-diphenyl-1,4-cyclohexadienecarboxylic acid Me ester (preparation given) reacted with PhCH2N(CH2OBu)(CH2SiMe3) in refluxing CF3CO2H to give the intermediate hexahydroisoindole derivative II.HCl, which was further cyclized by CF3SO3H at 5-20æ?to give the benz[f]isoindole intermediate III. This was then converted in 3 steps to title compound IV. In an assay for inhibition of farnesyl transferase, IV had an IC50 of 0.31 æ¸M. The experimental process involved the reaction of (S)-2-(2-Methoxyphenyl)propanoic acid(cas: 81616-80-0).SDS of cas: 81616-80-0
The Article related to benzisoindole preparation farnesyl transferase inhibitor antitumor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.SDS of cas: 81616-80-0
Referemce:
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Ether | (C2H5)2O – PubChem