Prepn. of (pyrimid-2-yl-thio- or seleno-) acetic acid derivs. - by reacting the corresp. chloro:alkanoyl-amino cpd. with a rhodanide and water or an alcohol

摘要

Prepn. of (pyrimid-2-ylthio or seleno)-ethanoic acid derivs. of formula (I) comprises reacting a cpd. of formula (II) with a cpd. of formula MXCN (III) and with a cpd. of formula HR2 (IV) with heating. In formulae, R1 is amino or OH; R2 is OH or 1-4C alkoxy; X is S or Se; A is a substd. aromatic ring condensed in the 4,5-position of the pyrimidine ring and opt. mono- or di-substd. with NO2, halo, Me or MeO, or A is a 5-7 membered heterocyclic ring, condensed in the 4,5-position of the pyridimine ring and opt. mono- or di-substd. with Me, methylamino, dimethylamino, MeS, ethanoyl, allyl, 1-4C alkoxy carbonyl tetramethylene, Ph, anilino or anilinocarbonyl, (these last 3 gps. are opt. substd. with halogen and/or MeO); Y is nitrile or 1-4C alkoxycarbonyl; Hal is halo, pref. Cl or Br; and M is NH4, Na or K. USE/ADVANTAGE - (I) are intermediates in organic syntheses, e.g., in the prepn. of pharmaceuticals. Some (I) are themselves pharmaceuticals.