112243-88-6Relevant academic research and scientific papers
Process for preparation of optically active N-mercaptoalkanoylamino acids
-
, (2008/06/13)
A process is disclosed wherein an optically active N-mercaptoalkanoylamino acid is prepared by (1) reacting an optically active β-hydroxyalkanoic acid, with a halogenating reagent to prepare an optically active β-haloalkanoyl halide (2) reacting the β-haloalkanoyl halide with an amino acid to produce an optically active N-β-haloalkanoylamino acid and (3) reacting the N-β-haloalkanoylamino acid with a reagent capable of converting the halogen into the thiol group, the configuration of the formulas (II), (III), (IV), (V), and (VI) being retained in all the optically active compounds throughout the process to prepare the compound represented by formula (I). The product of the present invention, for example, N-(3-mercapto-2-D-methylpropanoyl)-L-proline inhibits the enzymatic conversion of angiotensin I into angiotensin II and therefore is useful for relieving angiotensin-related hypertension.
Pyridinium salts
-
, (2008/06/13)
The invention concerns compounds of formula STR1 wherein the sulphur is bonded to the pyridinium ring at position 2 or 4, Y is --S-- or --CH2 --, R represents hydrogen, or a lower alkyl group, or other carboxylic protecting group; R1 represents hydrogen or lower alkyl; R2 represents lower alkyl, aryl of 6 to 10 carbon atoms or aralkyl of 7 to 11 carbon atoms; R3 represents hydrogen or a substituent selected from lower alkyl, halogen and lower alkoxy; q and r are each 1 or 2; and X? represents a halide ion or an organosulphonate ion, which are antihypertensive agents and are useful as intermediates to captopril and analogous compounds.
PROLINE DERIVATIVES AND RELATED COMPOUNDS
-
, (2008/06/13)
New proline derivatives and related compounds which have the general formula STR1 are useful as angiotensin converting enzyme inhibitors.
