| 摘要 |
<p>1368232 Azetidino-thiazolidine compounds GLAXO LABORATORIES Ltd 30 July 1971 [31 July 1970] 37187/70 Heading C2C Novel compounds of the formula in which R<SP>1</SP> is the residue of an acyl group R<SP>1</SP>CO- having 1-21 carbon atoms, R<SP>3</SP> is H, halocarbonyl or a selectively removable group serving to protect a secondary nitrogen atom, and R<SP>4</SP> is H or an esterified malonate group, or a group where R is a carboxyl group or esterified carboxyl group or a protected hydroxyl or amino group (e.g. an ether or methane group), may be obtained by reacting a compound of the formula with a reducing agent serving to reduce an imino-thioether to an amino-thioether, e.g. dissolving metal reducing agents such as Zn in acid or aluminium amalgam in the presence of water, optionally followed by reaction of the product (in which R 3 = H) with a reagent capable of introducing the protecting group, e.g. (i) by reaction with phosgene to form the compound in which R 3 is halocarbonyl then reacting the latter with an alcohol or phenol, or (ii) by reaction with a haloformic acid. The protecting groups may subsequently removed, e.g. by mild acidic or basic hydrolysis, enzymic hydrolysis or hydrogenolysis. Reference has been directed by the Comptroller to Specification 1,271,180.</p> |
