- Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-ones and intermediates thereof
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A process is provided for the preparation of compounds of formula (I) herein comprising reacting a compound of formula (II), (III), (IV) or (V) in the presence of-OR3 and a hydroxide trapping agent or in the case of compounds of formula (IV) reacting in the presence of an auxiliary base and a hydroxide trapping agent (i.e.-OR3 is substituted by the auxiliary base), wherein X is a leaving group and R1 to R4 are as defined.
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- Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
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Compounds of the formulae (IA) and (IB): wherein R1is C1to C3alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1to C4alkoxy; halo; CN; CF3; OCF3or C1to C4alkyl wherein said C1to C4alkyl group is optionally substituted by C1to C4haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2is C1to C6alkyl and R13is OR3or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
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- AN IMPROVED METHOD OF CHLORINATING 2-ALKOXYNICOTINIC ACIDS
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A novel chlorination process for preparing 5-chloro-2-alkoxynicotinic acids has been developed using commercial 5.25percent sodium hypochlorite (Clorox) as a chlorinating agent.
- Elliott, Mark L.,Goddard, Carl J.
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p. 1505 - 1508
(2007/10/02)
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- Hypoglycemic 5-substituted oxazolidine-2,4-diones
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Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2,4-diones and the pharmaceutically acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.
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