- ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON VASCULAR ENDOTHELIAL LIPASE
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Disclosed is a compound which is useful as an endothelial lipase inhibitor. A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: , its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by the formula: -C(R1R2)-C(=O)-NR3R4 and a group represented by the formula: -R5, a broken line represents the presence or the absence of a bond, Z is -NR6-, =N-, -O-, or -S-, R6 is halogen, substituted or unsubstituted alkyl or the like, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like.
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- Heterocyclizations with C-thiocarbamoyl-substituted derivatives of phosphonium ylides
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We found an easy method for conducting the Ph3P=C(X)H -> -> Ph3P=C(X)C(S)NH2 transformation that is based on treating accessible phosphonium ylides first with acetyl isothiocyanate and then with sodium hydroxide.New thiocarbamoyl-containing reagents readily enter into cyclocondensation with α-halocarbonyl compounds and chloroacetonitrile; this property was used for synthesizing a number of stabilized ylides of the general formula Ph3P=C(X)Ht.
- Smolii, O. B.,Panchishin, S. Ya.,Romanenko, E. A.,Drach, B. S.
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p. 521 - 524
(2007/10/03)
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