2 QUINOLINE THIO ACETAMIDES

• Main Authors: NOHARA A,JA, HONDA H,JA, KANAI Y,JA, SANNO Y,JA, KANNO M,JA
• Format: Patent
• Language: English
• Published: 08.10.1974
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

1285302 Thioacetamides TAKEDA YAKUHIN KOGYO KK 7 July 1970 [8 July 1969 27 Sept 1969] 32790/70 Heading C2C Novel compounds I (including salts thereof) where R 1 is H, alkyl, alkoxy or halogen, n is 1 to 4, including the case where (R 1 ) n signifies a divalent straight-chain hydrocarbon radical of 4C which is attached to the 5th and 6th positions of the pyridine ring, R 2 and R 3 are H, alkyl, aralkyl or aryl or together with the adjacent N comprise a heterocycle, and with the proviso that R 1 , R 2 and R 3 are not simultaneously H, are made: (a) by reacting a corresponding -CH 2 CONR 2 R 3 compound with a phosphorus sulphide, or with a halogenating agent and then reacting the product so obtained with hydrogen sulphide; (b) by reacting NHR1 2 R1 3 with a compound I containing the 2-CH 2 CSNH 2 group, to afford a corresponding I containing a 2-CH 2 CSNR1 2 R1 3 group (R1 2 and R1 3 are the same as R 2 and R 3 but are not simultaneously H); and (c) by reacting a corresponding compound with hydrogen sulphide, RCSNH 2 (R is alkyl, aryl or aralkyl) or (R1O) 2 P(:S)SH, to afford I containing the 2-CH 2 CS.NH 2 group, or with R 2 NH 2 followed by reaction of the product so obtained with hydrogen sulphide to afford a corresponding I containing a group (R1 is alkyl). Pharmaceutical preparations useful in treating and/or preventing gastric diseases contain I as active ingredient; suitable forms for administration are, e.g. powders, granules and tablets, and solutions for injection.