Skip to main content
. 2016 Jan 21;59(3):1078–1101. doi: 10.1021/acs.jmedchem.5b01685

Table 3. Introduction of Polarity at the Pyridine C-4 Substituent.

graphic file with name jm-2015-01685g_0003.jpg

graphic file with name jm-2015-01685g_0004.jpg

graphic file with name jm-2015-01685g_0005.jpg

a

Free base.

b

TFA salt.

c

The chloro substituent is at C-5 according to 5-(5-chloro-4-(1-methyl-1,8-diazaspiro[4.5]decan-8-yl)pyridin-3-yl)-1-methyl-1,3-dihydrobenzo[c]isothiazole 2,2-dioxide.

d

The chloro substituent is at C-5 according to 5-(5-chloro-4-(1-(2-methoxyethyl)-1,8-diazaspiro[4.5]decan-8-yl)pyridin-3-yl)-1-methyl-1,3-dihydrobenzo[c]isothiazole 2,2-dioxide.

e

The chloro substituent is at C-5 according to 5-(5-chloro-4-(1-(3-methoxypropyl)-1,8-diazaspiro[4.5]decan-8-yl)pyridin-3-yl)-1-methyl-1,3-dihydrobenzo[c]isothiazole 2,2-dioxide.

f

The chloro substituent is at C-5 according to 5-(5-chloro-4-(1-(3-(methylsulfonyl)propyl)-1,8-diazaspiro[4.5]decan-8-yl)pyridin-3-yl)-1-methyl-1,3-dihydrobenzo[c]isothiazole 2,2-dioxide.