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    • 4. 发明专利
    • PYRIDINE THIOACETAMIDE DERIVATIVES
    • CA939347A
    • 1974-01-01
    • CA87627
    • 1970-07-08
    • TAKEDA CHEMICAL INDUSTRIES LTD
    • KANAI YOSHIOKANNO MORIOSANNO YASUSHINOHARA AKIRAHONDA HARUOMI
    • C07D213/59C07D213/68C07D215/12
    • 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 NHR 1 2 R 1 3 with a compound I containing the 2-CH 2 CSNH 2 group, to afford a corresponding I containing a 2-CH 2 CSNR 1 2 R 1 3 group (R 1 2 and R 1 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 (R 1 O) 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 (R 1 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.