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Title: Synthesis of potent water soluble forskolin analogues
Authors: Lal, Bansi
Gangopadhyay, Ashok Kumar
Gidwani, Ramesh M
Rajagopalan, Ramanujam
Ghate, Anil V
Keywords: forskolin
water soluble
ω-halo acid
acrylic acid
hydroxyacyl forskolin
aliphatic amine
Michael addition
heterocyclic amine
inotropic activity
Issue Date: Jan-2006
Publisher: CSIR
Series/Report no.: <b>Int</b>.<b>Cl</b>.<b><sup>7</sup> C 07 C</b>
Abstract: The coupling of ω-halo acid or acrylic acid with 6<img src='/image/spc_char/beta.gif'>-2-hydroxyacyl forskolin <b style="">1</b> in the presence of DCC and DMAP gives 6<img src='/image/spc_char/beta.gif'>-ω-haloacyloxy or acryloxy derivatives <b style="">10</b>-<b style="">12</b>. These derivatives undergo halogen displacement or Michael addition reaction with aliphatic or heterocyclic amine to afford compounds <b style="">13</b>-<b style="">28</b>. Alternatively, <b style="">1</b> is coupled with N-trityl protected amino acid to give corresponding intermediates <b style="">2</b>-<b style="">5</b>. Removal of trityl group could be achieved by TFA diluted with ether and subsequent salt formation with HCl in ether yields <b style="">6</b>-<b style="">9</b> as hydrochloride salt. Compound <b style="">6</b> has shown excellent <i style="">in vitro</i> and <i style="">in vivo</i> positive inotropic activity.
Description: 232-246
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.45B(01) [January 2006]

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