Abstract:
Title compds. I(R1,R2 = H, OH; R3 = α- or β-thienyl, α- or β-thienylmethyl, benzo[b thiophene, cyclopentano[b thiopene, cyclohexano[b thiopene; X = C1-7 straight-or sidechain alkylene, C2-8 alkoxyalkylene), exhibiting a hypotension activity and a urination activity, were prepd. by the reaction of lactol (II) and 4-carboxy-butyl-triphenylphosphonium bromide in NaH-dissolved dimethylsulfoxide in the presence of inert gas to give formula acid(II), which was acid hydrolyzed to give compds. I or their esters by eliminating tetrahydropyranyl protecting group.
Abstract:
6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by (a) reacting, in an inert organic solvent, a salt of sulfamic acid, which is at least partially soluble therein, with at least approximately the equimolar amount of an acetoacetylating agent, in the presence of an amine or phosphine catalyst, and by cyclizing the acetoacetamide-N-sulfonate which is formed in this reaction, or the free sulfonic acid, (b) by the action of at least approximately the equimolar amount of SO3, where appropriate in an inert inorganic or organic solvent, to give 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide, which is produced in the form of the acid in this reaction; it is possible, if desired, to obtain from the acid form (c) the appropriate salts by neutralization with bases. The non-toxic salts - in particular the potassium salt - are valuable synthetic sweeteners.
Abstract:
6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2dioxide is prepared by reaction of acetoacetamide with at least approximately twice the molar amount of S03 per mole of acetoacetamide, if appropriate in an inert inorganic or organic solvent. Relevant salts can be obtained, using bases, from the product which results in the form of the acid. The non-toxic saLts, in particular the potassium salt, are valuable synthetic sweeteners.
Abstract:
6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared by reaction of acetoacetamide with at least approximately twice the molar amount of SO3 per mole of acetoacetamide, if appropriate in an inert inorganic or organic solvent. Relevant salts can be obtained, using bases, from the product which results in the form of the acid. The non-toxic salts, in particular the potassium salt, are valuable synthetic sweeteners.