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Indian Journal of Chemistry -Section B (IJC-B) >
IJC-B Vol.45B [2006] >
IJC-B Vol.45B(01) [January 2006] >
| 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 |
| IPC Code: | Int.Cl.7 C 07 C |
| Abstract: | The coupling of ω-halo acid or acrylic acid with 6 -2-hydroxyacyl forskolin 1 in the presence of DCC and DMAP gives 6-ω-haloacyloxy or acryloxy derivatives 10-12. These derivatives undergo halogen displacement or Michael addition reaction with aliphatic or heterocyclic amine to afford compounds 13-28. Alternatively, 1 is coupled with N-trityl protected amino acid to give corresponding intermediates 2-5. Removal of trityl group could be achieved by TFA diluted with ether and subsequent salt formation with HCl in ether yields 6-9 as hydrochloride salt. Compound 6 has shown excellent in vitro and in vivo positive inotropic activity. |
| Page(s): | 232-246 |
| ISSN: | 0975-0983(Online); 0376-4699(Print) |
| Source: | IJC-B Vol.45B(01) [January 2006]
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