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Part-A Studies on 2-methyl indoline derivatives…..
Kabbe et. al. 122 synthesized N-2-dimethyl indoline-1-carboxamide
(alkylurea) derivatives from 2-methyl indoline using methyl isocyanate for the
treatment of lipometabolic diseases / disorders.
Bermudez et. al. 123 reported that Indazole (1) is a potent and selective
5-HT3 receptor antagonist. On those basis, a novel series of potent 5-HT3
receptor antagonists, 1-indoline- and 1-indole carboxamides (2) [R = H , F, Cl,
OCH3, NO2; R 1 = H, methyl, ethyl, phenyl; R 2 = H, methyl; R 1 R 2 = (CH2)2,
(CH2)4, (CH2)5; R 3 = H, methyl; n = 2, 3] and (3) (R 1 = H, methyl, ethyl,
phenyl), respectively, were described. The activity of (2) suggested that
aromaticity of the 5-membered ring was not an essential requirement for the
potency provided that an in plane orientation of the CO group was favored.
On the basis of this hypothesis indene (4) was prepared. In (4) the in plane
orientation of the CO group was maintained by conjugation with the aromatic
ring through the sp 2 -hybridized C. (4) was also a potent 5-HT3 receptor
antagonist. (Fig. A.8 & 9)
Fig. A.8
Fig. A.9
Department of Chemistry, Saurashtra University, Rajkot – 360 005 21